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Attached to peptide or protein of 2+ amino acid units (e.g., dipeptide, folate, fibrinogen, transferrin, sp. enzymes); derivative thereof

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424 - Drug, bio-affecting and body treating compositions

424100110 - RADIONUCLIDE OR INTENDED RADIONUCLIDE CONTAINING; ADJUVANT OR CARRIER COMPOSITIONS; INTERMEDIATE OR PREPARATORY COMPOSITIONS

424100650 - In an organic compound

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DocumentTitleDate
20090098047BIOCONJUGATES OF METAL COMPLEXES OF NITROGEN-CONTAINING MACROCYCLIC LIGANDS - The present invention is directed to bioconjugates of complexes represented by the formula:04-16-2009
20090214424Human glycoprotein hormone superagonists and uses thereof - The present invention provides improved methods of imaging, targeted therapy and detection and diagnostics using modified glycoprotein hormones having increased activity over wild-type hormones.08-27-2009
20090317326RADIOFLUORINATION METHODS - The present invention relates to radiolabelled substitute benzene compounds for diagnostic imaging. The present invention provides methods for preparation of such compounds, in particular, preparation of novel compounds which serve as precursors for 12-24-2009
20080260638RECEPTOR(SSTR2)-SELECTIVE SOMATOSTATIN ANTAGONISTS - SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto.10-23-2008
20090004105Molecular imaging of matrix metalloproteinase expression using labeled chlorotoxin - Embodiments of the present disclosure provide for: methods for imaging MMP-2 positive tissue; methods of diagnosing the presence of one or more of MMP-2 positive precancerous cells, MMP-2 positive cancerous cells, MMP-2 positive tumor cells, and MMP-2 positive diseases in a tissue; method of monitoring the progress of one or more of MMP-2 positive precancerous cells, MMP-2 positive cancerous cells, MMP-2 positive tumor cells, and MMP-2 positive diseases in a tissue; pharmaceutical compositions for imaging one or more of MMP-2 positive precancerous cells, MMP-2 positive cancerous cells, MMP-2 positive tumor cells, and MMP-2 positive diseases; compositions; kits; and the like.01-01-2009
20100015051Transferrin-conjugated nanoparticles for increasing efficacy of a therapeutic agent - The present invention relates to a transferrin-conjugated nanoparticle composition with sustained release characteristics. A method for increasing the efficacy of therapeutic agents and a method for treating cancer using the transferrin-conjugated nanoparticle composition are also provided.01-21-2010
20090123371MOLECULAR SIGNATURE OF CANCER - The present invention provides compounds, compositions, and methods for detecting, diagnosing and treating cancers such as glioblastoma multiforme.05-14-2009
20090191124PDGF-RBeta BINDERS - Provided herein are PDGF-Rβ imaging agents that are polypeptides labeled with a signal generator (e.g., paramagnetic label, a radionuclide, or a fluorophore), wherein the imaging agents bind specifically to PDGFR-β. Also provided are in vivo imaging methods using the imaging agents.07-30-2009
20090191123NOVEL IMAGING AGENTS - The present invention provides a novel imaging agent suitable for the non-invasive visualization of fibrosis. A precursor for the preparation of the imaging agent is also provided by the invention, as well as a pharmaceutical composition comprising the imaging agent and a kit for the preparation of the pharmaceutical composition. In a further aspect, use of the imaging agent for in vivo imaging and in the preparation of a medicament for the diagnosis of a condition which comprises fibrosis is provided.07-30-2009
20100074844Cyclopeptides Containing RGD Mimetics As Imaging Markers For Integrins - Radiolabeled cyclic polypeptides, pharmaceutical compositions comprising radiolabeled cyclic polypeptides, and methods of using the radiolabeled cyclic polypeptides. Such polypeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).03-25-2010
20100074843Novel Substrate Based PET Imaging Agents - The present application is directed to radiolabeled imaging agents comprising a radiolabel, and a substrate, pharmaceutical compositions comprising radiolabeled imaging agents, and methods of using the radiolabeled imaging agents. The present application is further directed to methods of preparing the radiolabeled imaging agent. Such imaging agents can used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).03-25-2010
20120244070FIBRONECTIN TARGETING CONTRAST AGENT - Example systems and methods enhance contrast in MRI images. To facilitate imaging of atherosclerotic plaques, arterial and venous, cardiac, and even tumor tissues and fibrosis, a fibrin-fibronectin complex or disease-related fibronectin specific MRI contrast agent (CLPD) has a specific binding affinity for fibronectin.09-27-2012
20130039853EFFICIENT SYNTHESIS OF CHELATORS FOR NUCLEAR IMAGING AND RADIOTHERAPY: COMPOSITIONS AND APPLICATIONS - Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.02-14-2013
20090035215RADIOFLUORINATION - The present invention relates to novel compounds suitable for or already radiolabeled with 02-05-2009
20090155170ANNEXIN DERIVATIVES SUITABLE FOR PRETARGETING IN THERAPY AND DIAGNOSIS - The present invention provides methods and compositions for the treatment and diagnosis of diseases such as neoplastic diseases, neurodegenerative diseases, cardiovascular diseases, autoimmune diseases, and inflammatory diseases. The methods are based on the concept of pretargeting and include the administration of complexes comprising a recognizable compound A coupled to annexins, and the administration of complexes comprising of pharmaceutical or diagnostic compounds coupled to a compound B recognizing and binding to compound A to subjects. The compositions include annexins, annexin variants, that are not internalized by the target cells, derivatives thereof, and complexes thereof.06-18-2009
20090155169Glyco-molecular imaging method for grade classification of liver fibrosis and its glyco-molecular imaging agent thereof - The invention discloses one glyco-molecular imaging method for grade classification of liver fibrosis and its glyco-molecular imaging agent. The agent combining with glyco-molecular imaging method for liver targeting could be used to differentiate the grade of liver fibrosis and follow-up evaluation of the therapeutic effect.06-18-2009
2010004054399mTc-LABELED 19 AMINO ACID CONTAINING PEPTIDE FOR USE AS PHOSPHATIDYLETHANOLAMINE BINDING MOLECULAR PROBE AND RADIOPHARMACEUTICAL - With only 19 amino acids, Duramycin is the smallest known polypeptide that has a defined 3-dimensional binding structure. Duramycin binds Phosphatidylethanolamine (PtdE) at a 1:1 ratio with high affinity and exclusive specificity. As an abundant binding target, PtdE is a major phospholipid and accounts for about 20% of the phospholipid content in mammalian cellular membranes. PtdE is externalized to the surface of apoptotic cells, and also becomes accessible in necrotic cells due to compromised plasma membrane integrity. Given the unique physicochemical properties of Duramycin and the availability of PtdE in acute cell death, the goal of this study is to develop and evaluate 02-18-2010
20100143250COMPOUNDS FOR THE DIAGNOSIS OF APOPTOSIS - The present invention relates to a compound of general formula (I) below: Signal−Linker−Peptide (I) in which Signal represents a signal entity; Linker, which may or may not be present, represents a chemical bond and Peptide represents a peptide comprising an apoptosis-targeting peptide, the apoptosis-targeting peptide being chosen from the peptides having the formula below and the functional equivalents thereof: 06-10-2010
20130028836CHLOROTOXIN POLYPEPTIDES AND CONJUGATES AND USES THEREOF - Reduced lysine chlorotoxin polypeptides that may be used to generate single species conjugates of chlorotoxin. Conjugates comprising such chlorotoxin polypeptides and pharmaceutical compositions thereof. Methods of using such compositions and/or conjugates.01-31-2013
20100068139Methods of radiofluorination of biologically active vectors - The invention relates to conjugates of formula (V) or (VI): wherein X is —CO—NH—, —NH—, —O—, —NHCONH—, or —NHCSNH—; their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.03-18-2010
20130052132Method for Producing Radioactively Labeled Polypeptide - The present invention relates to a method for producing a polypeptide. The method includes labeling a molecular probe precursor represented by an amino acid sequence of the formula (1) using a labeling compound capable of labeling a lysine or lysine derivative:02-28-2013
20100135905ASSESSMENT OF CANCER SUSCEPTIBILITY TO MOLECULAR TARGETED THERAPY BY USE OF RECOMBINANT PEPTIDES - A method for assessing cancer susceptibility to molecular targeted therapy. Also provided are methods for in vivo panning of diverse molecules for isolation of targeting ligands that specifically bind an apoptotic cell associated with a responding tumor, targeting ligands identified by the panning methods, and diagnostic and imaging uses therefor.06-03-2010
20090311177Radiolabelling Methods - The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II): R*-L2-N12-17-2009
20130089500ANTAGONISTS OF LIGANDS AND USES THEREOF - The invention provides multivalent ligand binding agents (traps) for members of the TGF-β superfamily and polypeptide linkers and methods for making and using such constructs. The traps may be used as therapeutic or diagnostic (imaging or non-imaging) agents for diseases/disorders caused by over-production/activity of the target ligand. In an embodiment of the invention there is provided a multivalent binding agent with affinity for a member of the TGF-β superfamily, the agent having the general structure I:04-11-2013
20130089499ANTAGONISTS OF LIGANDS AND USES THEREOF - The invention provides multivalent ligand binding agents (traps) for members of the TGF-β superfamily and polypeptide linkers and methods for making and using such constructs. The traps may be used as therapeutic or diagnostic (imaging or non-imaging) agents for diseases/disorders caused by over-production/activity of the target ligand. In an embodiment of the invention there is provided a multivalent binding agent with affinity for a member of the TGF-β superfamily, the agent having the general structure I:04-11-2013
20130089498COMPOSITIONS AND METHODS RELATED TO PROFILING A PLURALITY OF CELLS BASED ON PEPTIDE BINDING - Methods and compositions are described for classifying cells and/or peptides that associate or bind with a particular characteristic pattern to a plurality of cells or cell lines. Aspects of the invention also include the use of peptide(s) having an appropriate binding characteristic to deliver a drug to a cell or cell population.04-11-2013
20090304586Chelating Agent Conjugated Alpha-MSH Peptide Derivatives, Preparation Method Thereof and Composition for Diagnosis and Treatment of Melanoma Comprising the Same as an Active Ingredient - Disclosed are chelating agent-conjugated α-MSH peptide derivatives, preparation methods thereof, and compositions for use in a diagnosis or treatment of a melanoma tumor containing the same as an active ingredient. The novel α-MSH peptide derivatives conjugated with chelating agent according to the present invention are highly selective to the melanocortin-1 receptor which is α-MSH receptor expressing in melanoma tumor and their labeling rate of a radioactive isotope is high. Also, they remain in kidney shortly and have high taking rate of the melanoma tumor. Therefore, with the aforesaid reasons, they may be effectively used for early diagnosis or treatment of melanoma tumor.12-10-2009
20090041661MEASUREMENT OF BIOSYNTHESIS AND BREAKDOWN RATES OF BIOLOGICAL MOLECULES THAT ARE INACCESSIBLE OR NOT EASILY ACCESSIBLE TO DIRECT SAMPLING, NON-INVASIVELY, BY LABEL INCORPORATION INTO METABOLIC DERIVATIVES AND CATABOLITIC PRODUCTS - Methods of determining rate of biosynthesis or breakdown of biological molecules from metabolic derivatives and catabolic products are disclosed herein. In particular, methods of measuring the rates of biosynthesis and breakdown of biological molecules inaccessible or not easily accessible to direct sampling by sampling metabolic derivatives and catabolic products in accessible biological samples are disclosed herein.02-12-2009
2013005886599mTc-LABELED 19 AMINO ACID CONTAINING PEPTIDE FOR USE AS PHOSPHATIDYLETHANOLAMINE BINDING MOLECULAR PROBE AND RADIOPHARMACEUTICAL - The invention encompasses radiopharmaceutical compounds that can be used in imaging cell death associated with either apoptosis or necrosis. Phosphatidylethanolamine (PtdE) is externalized to the surface of apoptotic cells, and also becomes accessible in necrotic cells due to compromised plasma membrane integrity. Duramycin, a 19 amino acid polypeptide, binds PtdE at a 1:1 ratio with high affinity and exclusive specificity. Novel Duramycin-based radiopharmaceuticals and non-radioactively labeled compounds are disclosed herein. Such compounds facilitate detection of cell apoptosis and/or necrosis by binding to PtdE. The location of the bound compound can then be pinpointed using standard imaging techniques.03-07-2013
20090285753Novel haptotactic peptides - Novel cell attachment peptides having sequences homologous to specific portions of the carboxy terminal sequence of fibrinogen chains are disclosed. The novel peptides, derived from proteins related to fibrinogen including a peptide adjacent to fibrinogen γ-chain C terminus denoted pre-Cγ possess cell attraction activities, and are useful in pharmaceutical compositions.11-19-2009
20110064659GLUTAMINE BIOMARKERS FOR DEPRESSION - Differential expression of nucleic acids in the brains of subjects suffering from late-onset depression has been demonstrated. The invention provides methods useful in the determination of late-onset depression. Also provided by the present invention is a screening method for the identification of compounds for treatment, prevention or diagnosis of late-onset depression.03-17-2011
20090068104Substantially Homogeneous Bio-Affecting Material Having a Pre-Determined Ratio of Bioaffecting Component to Cell Targeting Component, the Method for Making Such a Material and the Method of its use - A homogeneous conjugate for targeting and treating diseased cells wherein the conjugate has a predetermined ratio of drug molecules to protein molecules that preferentially bind to such cells and a method for making such a conjugate. The method of making the conjugate comprises adding drug molecules to linker molecules in a manner that effectively results in one molecule of drug for each molecule of linker followed by the addition of the drug-linker combination to protein molecules in order to achieve the predetermined ratio of drug molecules to protein molecules.03-12-2009
20120225016COMPOUNDS WITH REDUCED RING SIZE FOR USE IN DIAGNOSING AND TREATING MELANOMA, INCLUDING METASTATIC MELANOMA AND METHODS RELATED TO SAME - The present invention is directed to novel non-invasive diagnostic tools/compounds to image cancers, especially, melanoma, including metastatic melanoma in vivo. The present compounds exhibit enhanced uptake in cancerous cells and tissue and decreased renal uptake in kidney, evidencing favorable pharmacokinetics of compounds of the present invention. The compounds according to the present invention represent an advance in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are also useful for initiating therapy for melanoma as well as monitor patients' response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.09-06-2012
20130064765ANTITHROMBOTIC NANOPARTICLE - The present invention encompasses an antithrombotic nanoparticle.03-14-2013
20130064766TRICARBONYL TECHNETIUM-99m OR RHENIUM-188 LABELED CYCLIC RGD DERIVATIVES, A PREPARATION METHOD THEREOF, AND A PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVES AS AN ACTIVE INGREDIENT FOR USE IN THE DIAGNOSIS OR TREATMENT OF ANGIOGENESIS-RELATED DISEASES - The present invention relates to tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives, a preparation method thereof, and a pharmaceutical composition containing the derivative as an active ingredient for use in the diagnosis or treatment (radiotherapy) of angiogenesis-related diseases. The tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives of the present invention has a high subnanomolar affinity to integrin α03-14-2013
20090257950Membrane Scaffold Proteins - The membrane scaffold proteins (MSP) of the present invention assemble with hydrophobic or partially hydrophobic proteins to form soluble nanoscale particles which preserve native structure and function; they are improved over liposomes and detergent micelles, both in terms of stability and preservation of biological activity and native conformation. In the presence of phospholipid, MSPs form nanoscopic phospholipid bilayer disks, with the MSP stabilizing the particle at the perimeter of the bilayer domain. The particle bilayer structure allows manipulation of incorporated proteins in solution or on solid supports, including for use with such surface-sensitive techniques as scanning probe microscopy or surface plasmon resonance. The nanoscale particles, which are robust in terms of integrity and maintenance of biological activity of incorporated proteins, facilitate pharmaceutical and biological research, structure/function correlations, structure determinations, bioseparations, and drug discovery.10-15-2009
20080260637Methods of Detecting Prostate Cancer - A method of detecting presence or absence of prostate cancer in a subject, both in vivo and ex vivo is disclosed. The method comprises analyzing mitochondria or a mitochondrial component in at least one prostate cell of the subject, whereby mitochondria an alteration in quantity and or characteristic is indicative of the presence or absence of the prostate cancer in the subject.10-23-2008
20090285754PEPTIDES FOR TARGETING APOPTOTIC CELLS AND USES THEREOF - The present invention relates to a peptide capable of specifically targeting apoptotic cells undergoing apoptosis and a use thereof. More particularly, it relates to a peptide having an amino acid sequence represented by anyone selected from the group consisting of SEQ ID NO: 1 to SEQ ID NO: 12 and targeting apoptotic cells, a composition for detection of apoptotic cells comprising the same as an effective ingredient, a composition for drug delivery comprising the same as an effective ingredient, a composition for imaging comprising the same as an effective ingredient and the like. The peptide of the present invention effectively detects apoptosis which is involved in tissues of neoplastic disease, myocardial infarction, stroke and arteriosclerosis. Accordingly, the peptide of the present invention may be used in imaging of diagnosis of the said diseases and reaction against a drug by binding imaging reagent and etc. as well as in protection and treatment for the said diseases by binding a treatment reagent and then delivering drug selectively.11-19-2009
20120114557Methods for Collagen Imaging - Diagnostic compositions and methods for imaging and/or assessing collagen are described. The diagnostic compositions can include collagen binding peptides.05-10-2012
20090175786Gastrin Releasing Peptide Compounds - New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure:07-09-2009
20120237443FUNCTIONALIZING IMPLANTABLE DEVICES WITH A POLY (DIOL CITRATE) POLYMER - The present invention is directed to a novel poly (diol citrates)-based coating for implantable devices. More specifically, the specification describes methods and compositions for making and using implantable devices coated with citric acid copolymers or citric acid copolymers impregnated with therapeutic compositions and/or cells.09-20-2012
20090104117COMPOSITIONS AND METHODS OF USE OF TARGETING PEPTIDES AGAINST PLACENTA AND ADIPOSE TISSUES - The present invention concerns compositions comprising and methods of identification and use of targeting peptides for placenta or adipose tissue. In certain embodiments, the targeting peptides comprise part or all of SEQ ID NO:5-11, SEQ ID NO:13-22 or SEQ ID NO:144. The peptides may be attached to various therapeutic agents for targeted delivery. Adipose-targeting peptides may be used in methods for weight control, inducing weight loss and treating lipodystrophy syndrome. Adipose-targeting may also be accomplished using other binding moieties selectively targeted to adipose receptors, such as a prohibitin receptor protein complex. Placenta-targeting peptides may be used to interfere with pregnancy, induce labor and/or for targeted delivery of therapeutic agents to placenta and/or fetus. In other embodiments, receptors identified by binding to placenta-targeting peptides may be used to screen compounds for potential teratogenicity. An exemplary placental receptor is FcRn/β04-23-2009
20090123370ALPHAVBETA6 PEPTIDE LIGANDS AND THEIR USES - AVβ6 peptide ligands, functional variants thereof and their nucleic acids encoding them are disclosed with their uses in the treatment and imaging of AVβ6 mediated diseases.05-14-2009
20100322856Compositions and Methods for Inducing Angiogenesis - An isolated peptide comprising an amino acid sequence HWRR as set forth by SEQ ID NO:5, the peptide consists of 4 or 5 amino acids, is provided. Also provided are methods of treating angiogenesis-related pathologies using the peptide of the invention or pharmaceutical compositions comprising same.12-23-2010
20100129289COMPOSITIONS AND METHODS FOR THE DETECTION OF VULNERABLE PLAQUE - Targeting polypeptide imaging agents, methods employing the agents, and kits employing the agents are provided. The targeting polypeptide imaging agents may have at least one targeting polypeptide and at least one contrast enhancing imaging agent.05-27-2010
20090246133METHODS AND COMPOSITIONS RELATED TO INTERNALIZING RGD PEPTIDES - Disclosed are compositions and methods useful for targeting tissue undergoing angiogenesis or to cells or tissue expressing αv integrins. The compositions and methods are based on peptide sequences that selectively bind to and home to tissue undergoing angiogenesis or to cells or tissue expressing αv integrins in animals. The disclosed targeting is useful for delivering therapeutic and detectable agents to tissue experiencing angiogenesis or to cells or tissue expressing αv integrins.10-01-2009
20110280802Linkers For Radiopharmaceutical Compounds - A new and improved method for extending the half life of pharmaceutical compounds for use in diagnostic imaging or therapy uses a novel linker to attach a diagnostic or therapeutic moiety to a targeting peptide or another diagnostic or therapeutic moiety. The resulting compound may have the general formula M-N—O—P-Q, wherein M is the diagnostic or therapeutic moiety, N—O—P is the linker of the present invention, and Q is the targeting peptide. In another embodiment the compounds may have the formula M-N—O—P-M, wherein M is independently a diagnostic or therapeutic moiety and N—O—P is the linker of the invention. Methods for imaging or treating a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound are further provided. Methods for radiotherapy of a patient using the compounds are further provided, as are methods for preparing a radiotherapeutic agent from the compounds.11-17-2011
20100196271Cage-Like Bifunctional Chelators, Copper-64 Radiopharmaceuticals and PET Imaging Using the Same - Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula08-05-2010
20100215575Systemic Administration of Chlorotoxin Agents for the Diagnosis and Treatment of Tumors - The present invention is directed to methods and compositions for the treatment and diagnosis of neoplastic tumors. The inventive methods generally include systemic (e.g., intravenous) administration of a chloroxotoxin agent that may or may not be labeled.08-26-2010
20100266499CYTOKINE RECEPTOR ZCYTOR17 MULTIMERS - Novel polypeptide combinations, polynucleotides encoding the polypeptides, and related compositions and methods are disclosed for zcytor17-containing multimeric or heterodimer cytokine receptors that may be used as novel cytokine antagonists, and within methods for detecting ligands that stimulate the proliferation and/or development of hematopoietic, lymphoid and myeloid cells in vitro and in vivo. The present invention also includes methods for producing the multimeric or heterodimeric cytokine receptor, uses therefor and antibodies thereto.10-21-2010
20120107237ARG-GLY-ASP-CONJUGATED ALPHA-MELANOCYTE STIMULATING HORMONE HYBRID PEPTIDE FOR USE IN DIAGNOSING AND TREATING MELANOMA, INCLUDING METASTATIC MELANOMA AND METHODS RELATED TO SAME - The present invention is directed to novel non-invasive diagnostic and therapeutic tools/compounds comprising a hybride cyclic peptide which utilizes a cyclic peptide chelating group wherein the compound binds to a MSH receptor to image and treat cancers, especially, melanoma, including metastatic melanoma in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probes are capable of detecting cancerous melanoma cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention will also be useful to initiate therapy for melanoma as well as monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compound according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.05-03-2012
20110300071TARGETING NPR-C IN ANGIOGENESIS AND ATHEROSCLEROSIS WITH A C-TYPE ATRIAL NATRIURETIC FACTOR (CANF)-COMB NANOCOMPLEX - Tracers are disclosed comprising an amphiphilic comb-like nanostructure conjugated with an oligopeptide such as a fragment of a natriuretic peptide, and a signaling moiety such as a positron-emitting radionuclide. A fragment of a natriuretic peptide comprises Arg-Ile-Asp-Arg-Ile (SEQ ID NO:1). Further disclosed are methods of imaging distribution of C-type atrial natriuretic peptide receptors and methods of imaging angiogenesis and atherosclerosis by PET scanning or MRI using a tracer.12-08-2011
20110300070BIOMOLECULE COMPLEXES AS CONTRAST AGENTS IN POSITRON EMISSION TOMOGRAPHY (PET) BASED METHODS FOR THE ASSESSMENT OF ORGAN FUNCTION - The present invention relates to complexes comprising one or more markers and one or more biomolecules for use as a contrast agent in positron emission tomography based imaging. The complexes according to the present invention preferably accumulate in a target compartment, such as the kidney. The present invention further relates to methods for generating the complexes and methods for using the complexes such as for evaluation of different aspects of kidney functionality e.g. for calculation of total and/or regional glomerular filtration rate in the kidney without the need for sampling blood or urine.12-08-2011
20110286920COMPLEX OF BIFUNCTIONAL CHELATING AGENT AND MANNOSYL HUMAN SERUM ALBUMIN - The present invention is about bifunctional chelating agents (BCA) conjugated mannosyl human serum albumin (MSA) and its radioisotope labeled compounds for imaging immune system such as macrophages, Kupffer cells, reticuloendothelial system (RES), and lymphatic system. The present invention comprises BCA-MSA conjugates, their radiolabeled compounds, and kits for radiolabeing. The present invention improved radiolabeling procedure, showed higher lymphatic system uptake, and enabled image by positron emission tomography (PET).11-24-2011
20110293516COMPOSITIONS AND METHODS OF USE OF TARGETING PEPTIDES AGAINST PLACENTA AND ADIPOSE TISSUES - The present invention concerns compositions comprising and methods of identification and use of targeting peptides for placenta or adipose tissue. In certain embodiments, the targeting peptides comprise part or all of SEQ ID NO:5-11, SEQ ID NO:13-22 or SEQ ID NO:144. The peptides may be attached to various therapeutic agents for targeted delivery. Adipose-targeting peptides may be used in methods for weight control, inducing weight loss and treating lipodystrophy syndrome. Adipose-targeting may also be accomplished using other binding moieties selectively targeted to adipose receptors, such as a prohibitin receptor protein complex. Placenta-targeting peptides may be used to interfere with pregnancy, induce labor and/or for targeted delivery of therapeutic agents to placenta and/or fetus. In other embodiments, receptors identified by binding to placenta-targeting peptides may be used to screen compounds for potential teratogenicity. An exemplary placental receptor is FcRn/β12-01-2011
20110293517Nitrogen-Containing Macrocyclic Conjugates As Radiopharmaceuticals - The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.12-01-2011
20090324497Tc and Re Labeled Radioactive Glycosylated Octreotide Derivatives - Improved sst-receptor binding peptidic ligands for diagnostic and therapeutic applications in nuclear medicine are provided. The improved ligands contain either natural or unnatural amino acids or peptidomimetic structures that are modified at either the N-terminal or the C-terminal end or at both termini, a carbohydrate unit and a chelator or prosthetic group to provide a complexation of a radioisotope binding or holding the radioisotope. The sst- or SSTR-receptor binding peptidic ligands may also contain one or more multifunctional linker units optionally coupling the peptide, and/or the sugar moiety and/or the chelator and/or the prosthetic group. Upon administering the ligand to a mammal through the blood system the ligand provides improved availability, clearance kinetics, sst-receptor targeting and internalization over the non-carbohydrated ligands.12-31-2009
20100055035BISAMINOETHANETHIOL-TARGETING LIGAND CONJUGATES AND COMPOSITIONS - The invention provides, in a general sense, a new labeling strategy employing 03-04-2010
20110217233MODULATION OF INTRACELLULAR SIGNALING - A method of treating a disease characterized by aberrant cell migration and/or invasion includes administering to a subject an effective amount of the peptide of SEQ ID NO:3, an Å6 polypeptide, or an isolated polypeptide consisting essentially of the Link region of human CD44 as indicated in FIG. 09-08-2011
20090148382Technetium- and rhenium-bis(heteroaryl) complexes, and methods of use thereof - One aspect of the invention relates to complexes of technetium (Tc) and rhenium (Re) with various heteroaromatic ligands, e.g., quinolinyl and isoquinolinyl ligands, and their use in fluorescence and radioimaging for a variety of clinical diagnostic applications, as well as radiopharmaceuticals for therapeutic applications. Another aspect of the invention relates to quinolinyl and isoquinolinyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium and rhenium complexes are also described. Another aspect of the invention relates to quinolinyl and isoquinolinyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.06-11-2009
20100119446SPECIFIC AND HIGH AFFINITY BINDING PROTEINS COMPRISING MODIFIED SH3 DOMAINS OF FYN KINASE - The present invention relates to a recombinant binding protein comprising at least one derivative of the Src homology 3 domain (SH3) of the FYN kinase, wherein at least one amino acid in or positioned up to two amino acids adjacent to the src loop and/or at least one amino acid in or positioned up to two amino acids adjacent to the RT loop is substituted, deleted or added. Furthermore, the invention is directed to fusion proteins comprising a binding protein according to the invention fused to a pharmaceutically and/or diagnostically active component. In addition, the invention concerns nucleotides coding for these binding and/or fusion proteins as well as corresponding vectors and host cells. Last but not least, the present invention relates to the use of binding and/or fusion proteins of the present invention for preparing a medicament or a diagnostic means as well as to pharmaceutical or diagnostic compositions comprising said binding and/or fusion proteins.05-13-2010
20080247947High dose 111In-pentetreotide therapy of neuroendocrine tumors - A method for treating a neuroendocrine tumor is disclosed, which includes administering a first dose of 10-09-2008
20100119445PLEXIN D1 AS A TARGET FOR TUMOR DIAGNOSIS AND THERAPY - The present invention relates to plexin D1 for use as a targetable protein in the treatment or diagnosis of disorders that involve expression of plexin D1. Diagnosis is suitably effected by detecting the presence of plexin D1 in the body or a bodily tissue or fluid, whereas treatment is effected by targeting plexin D1 for delivery of therapeutics to the site where treatment is needed. The invention further relates to the use of molecules that bind plexin D1, a nucleic acid encoding plexine D1 or a ligand of plexin D1 for the preparation of a therapeutical composition for the treatment or diagnosis of disorders that involve expression of plexin D1. The disorders comprise disorders in which plexin D1 is expressed on tumor cells, tumor blood vessels or activated macrophages.05-13-2010
20100086480LOW RADIOCARBON DIETARY SUPPLEMENTS AND METHODS OF MAKING SAME - Methods for significantly lowering the carbon-14 content, particularly of DNA and histones in vertebrates, especially humans, to significantly below normal background levels and thereby reduce chromosomal damage using dietary supplements based on low radiocarbon DNA and histone precursors optionally including selected low radiocarbon amino acids, preferably including those which contribute the largest share of histone carbon atoms. Administration of the supplements during the earliest and/or most active growth stages of life is particularly beneficial. Components of the low radiocarbon supplements can be produced using a photobioreactor, an aqueous reaction medium and low radiocarbon carbon dioxide. The photobioreactor can be integrated into a body of water or can comprise a mobile, floating structure. Low radiocarbon by-products of photosynthesis can be recycled for use in non-photosynthetic fermentation processes to increase the yield of desirable supplement components.04-08-2010
20090263320Peptide-Based Compounds - The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise targeting vectors which bind to integrin receptors.10-22-2009
20110171129Molecular Probe Precursor for Imaging of Pancreatic Islet, and Use Thereof - A precursor of a molecular probe for imaging of pancreatic islets is provided. The precursor includes a polypeptide represented by any one of the following formulae (1) to (12), or a polypeptide having a homology with the foregoing polypeptide:07-14-2011
20110171128APROTININ POLYPEPTIDES FOR TRANSPORTING A COMPOUND ACROSS THE BLOOD-BRAIN BARRIER - The invention relates to improvements in the field of drug delivery. More particularly, the invention relates to polypeptides derived from aprotinin and from aprotinin analogs as well as conjugates and pharmaceutical compositions comprising these polypeptides or conjugates. The present invention also relates to the use of these polypeptides for transporting a compound or drug across the blood-brain barrier of a mammal and in the treatment and diagnosis of neurological diseases.07-14-2011
20080206136Binding Peptidomimetics and Uses of the Same - A multimeric peptidomimetic that comprises two or more monomers is disclosed. The monomers comprise an exocyclic peptide comprising a ring structure, a flexible linker sequence and a multimeric motif. Use of the monomers, a nucleic acid molecule encoding monomers, recombinant expression vectors comprising the nucleic acid molecule and host cells comprising a recombinant expression vector are disclosed. Methods of delivering a drug, a toxin, a nucleic acid molecule, a radionuclide or a detectable compound to a cell are disclosed.08-28-2008
20090274623IN VIVO IMAGING AGENTS FOR MET RECEPTOR TYROSINE KINASE - Provided are in vivo imaging agents comprising muteins of hTLc having detectable binding affinity for c-Met or a domain thereof, coupled to a signal generator, and the mutein coupled to a signal generator is disposed in a pharmaceutically acceptable carrier. Also provided are diagnostic methods using in vivo imaging agents comprising muteins of hTLc having detectable binding affinity for c-Met or a domain thereof.11-05-2009
20090291049Targeted delivery to human diseases and disorders - The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.11-26-2009
20080311036Imaging of Neural and Organ Injury or Damage - In vivo determination of regional damage with neural and organ injury specific imaging agents. Rapid, and non-invasive imaging compositions and methods for assessment of the extent of neurotoxic cell loss or nervous system damage resulting from nervous system injury due to ischemia, stroke, trauma, chemical or electrical insult, acute drug overdose or exposure to substance abuse (such as “recreational drugs”) infection or other insults. The same or similar rapid, and non-invasive imaging compositions and methods for assessment of the extent of the organ injury comprises any damage, injury or infection, functional failure to specific organs such as liver, kidney, prostate, lung, skeletal muscle, heart, pancreas, stomach, small and large intestine, bladder and the reproductive system as well as damage, injury or infection, functional failure to multi-organs, trauma-hemorrhagic shock and sepsis. In particular, neural and organ damage is detected via protease inhibitor-based radionuclide-labeled imaging ligand binding to overactivated proteases (calpains, caspases, cathepsins, proteasome, metalloproteases, granzyme B or other proteases) that are specific to neural or organ injury or damage.12-18-2008
20100061929NEOPLASIA TARGETING PEPTIDES AND METHODS OF USING THE SAME - The present invention provides compositions including neoplasia targeting peptides as well as methods of using the neoplasia targeting peptides in diagnosing, detecting, treating, monitoring treatment, and analyzing cancer or cancer cells in vivo and in vitro.03-11-2010
20100061930ErbB-2 RECEPTOR TARGETING PEPTIDE - The ErbB-2 receptor, a member of the tyrosine kinase type 1 family of receptors, has been implicated in many human malignancies. Bacteriophage display technology was employed to identify peptides that bound to the extracellular domain of human ErbB-2. The peptide KCCYSL, most frequently occurring in the affinity selected population, was chemically synthesized and characterized for its binding activities to the recombinant extracellular domain of ErbB-2. The synthetic peptide exhibits high specificity to ErbB-2 as well as to ErbB-1, another member of ErbB family. Thus, this peptide can be employed in cancer imaging or therapeutic agent targeting to malignant cells ErbB-2 receptor.03-11-2010
20080213176Compositions for Targeting Amine Oxidases in Vivo - This invention relates to a diagnostic compositions for targeting an amine oxidase enzyme in vivo, said composition comprising a labelled peptide having the capability to bind to said enzyme. Further, the invention concerns a pharmaceutical composition for use to modulate the activity of an amine oxidase enzyme, said composition comprising a peptide having the capability to bind to said enzyme, wherein said peptide further is conjugated to a therapeutically active agent. Still further, the invention concerns a novel peptide and its uses, especially as VAP-1 inhibitor.09-04-2008
20110206605Molecular Probe for Imaging of Pancreatic Islets and Use of the Same - A molecular probe for use in imaging of pancreatic islets is provided. The molecular probe comprises a polypeptide represented by the following formula (1), (2), or (3), or a polypeptide having homology with the foregoing polypeptide,08-25-2011
20080274052RADIOFLORINATION METHODS - The present invention relates to methods and reagents for [11-06-2008
20080274051Diagnosis and Treatment of Mood Disorders - The present invention relates to the diagnosis, treatment and monitoring of mood disorders. For example, a diagnosis may be performed by determining whether a monoamine oxidase in a vertebrate is elevated compared to a healthy control subject. Methods of monitoring treatments and methods for identifying treatments for mood disorders are also provided.11-06-2008
20080274050Labelled Adrenomedullin Derivatives and Their Use for Imaging and Therapy - The present invention relates to an adrenomedullin derivative including an adrenomedullin peptide chelated with at least one active agent. Examples of active agents include a paramagnetic element, a radioactive element and a fibrinolytic agent, among others. Paramagnetic agents have a distribution that is relatively easily shown through Magnetic Resonance Imaging (MRI). Radioactive agents have applications in imaging and delivery of radiations, depending on the specific element included in the active agent. Delivery of fibrinolytic agents mainly to a specific organ, such us for example to the lungs, allows to substantially improve the specificity and efficacy of thrombolytic therapy by allowing local delivery of the fibrinolytic agent, thereby reducing the risks of major bleeding in the therapy of the organ. If the organ is the lungs, a non-limiting example of pathology treatable with the fibrinolytic is pulmonary embolus.11-06-2008
20090297444PEPTIDE ANALOGS OF ALPHA-MELANOCYTE STIMULATING HORMONE - Provided herein are stable peptide analogs of the native alpha-melanocyte stimulating hormone (α-MSH) having selectivity for the melanocortin 1 receptor (MC1R). Also provided herein are pharmaceutical preparations of the α-MSH peptide analogs, as well as methods of using these analogs in the treatment of medical and veterinary conditions involving MC1R.12-03-2009
20100196270RADIOFLUORINATION METHODS - The invention relates to conjugates of formula (V) or (VI), their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.08-05-2010
20120294802USE OF ANTI-CGRP ANTIBODIES AND ANTIBODY FRAGMENTS TO PREVENT OR INHIBIT PHOTOPHOBIA OR LIGHT AVERSION IN SUBJECTS IN NEED THEREOF, ESPECIALLY MIGRAINE SUFFERERS - The present invention is directed to methods of inhibiting or preventing photophobia in subjects in need thereof using anti-CGRP antibodies or antibody fragments that inhibit photophobia, especially CGRP-associated photophobia. These antibodies and fragments are useful in treating different disorders associated with photophobia such as migraine, cluster headaches and the like.11-22-2012
20080213174Radiolabelled Insulin - The invention relates to in vivo imaging agents, specifically radiolabelled insulin derivatives of formula (III); wherein X is —CO—NH—, —NH—, —O—, —NHCONH—, or —NHCSNH—, and is preferably —CO—NH—, —NH— or —O—; Y is H, alkyl or aryl substituents; R* is a radiolabel moiety suitable for detection by SPECT or PET; and methods for preparing the same as well as their use in in vivo imaging methods.09-04-2008
20110206606STABLE RADIOPHARMACEUTICAL COMPOSITIONS AND METHODS FOR PREPARATION - Stabilized radiopharmaceutical formulations are disclosed. Methods of making and using stabilized radiopharmaceutical formulations are also disclosed. The invention relates to stabilizers that improve the radiostability of radiotherapeutic and radiodiagnostic compounds, and formulations containing them. In particular, it relates to stabilizers useful in the preparation and stabilization of targeted radiodiagnostic and radiotherapeutic compounds, and, in a preferred embodiment, to the preparation and stabilization of radiodiagnostic and radiotherapeutic compounds that are targeted to the Gastrin Releasing Peptide Receptor (GRP-Receptor).08-25-2011
20080292549High Affinity Melan-A T Cell Receptors - The present invention provides TCRs having an affinity (K11-27-2008
20120294801CONJUGATES OF RGD PEPTIDES AND PORPHYRIN OR (BACTERIO)CHLOROPHYLL PHOTOSYNTHESIZERS AND THEIR USES - Conjugates of porphyrin, chlorophyll and bacteriochlorophyll photosensitizers with RGD-containing peptides or RGD peptidomimetics are provided that are useful for photodynamic therapy (PDT), particularly vascular-targeted PDT (VTP), of tumors and nonneoplastic vascular diseases such as age-related macular degeneration, and for diagnosis of tumors by different techniques.11-22-2012
20110027175CANCER IMAGING AND TREATMENT - A compound, or a pharmaceutically acceptable salt or ester thereof, comprises a ligand for the chemokine receptor CXCR4 and a detectable label, the ligand having a binding affinity for the CXCR4 receptor, measured as IC02-03-2011
20090304585Stabilized Compositions and Methods for Radiolabeling Pharmaceuticals with Alpha-Particle Emitters - Oxidants (e.g., N-chlorosuccinimide) can be used to stabilize α-particle emitters (e.g., 12-10-2009
20090136420Neoplasm-specific polypeptides and their uses - The present invention features novel polypeptides and methods of using these polypeptides in the diagnosis, detection, monitoring, and treatment of neoplasms in a mammal, e.g., a human.05-28-2009
20090136421PAI-2 conjugates for the treatment and imaging of cancer - A method is described for detecting, visualizing, or treating cells, particularly cancerous cells, that express a uPA/uPAR complex. The method employs a PAI-2 conjugate molecule that comprises PAI-2 or a functional derivative, homologue, analogue, chemical equivalent or mimetic thereof, which PAI-2 is bound, linked, or otherwise associated with a toxin or label.05-28-2009
20090208412Contrast Agents - A contrast agent of the general formula (I): Z08-20-2009
20090169473DIAGNOSTIC AGENT AND THERAPEUTIC AGENT FOR DISEASE ASSOCIATED WITH HEPATOCYTE GROWTH FACTOR RECEPTOR - Disclosed is a diagnostic agent which is useful for imaging the site of application at which the highest therapeutic effect is expected (i.e., the site where an HGF receptor is expressed) in the therapy of an ischemic disease with an HGF plasmid for the purpose of promoting the angiogenesis with good efficiency.07-02-2009
20100150834HIGH AFFINITY EPHB RECEPTOR BINDING COMPOUNDS AND METHODS OF USE THEREOF - The present invention provides peptide-based compounds that selectively bind to a member(s) of the EphB receptor family, including, but not limited to, EphB1, EphB2, EphB3, EphB4, EphB5 and EphB6. In particular, the invention provides multimeric peptides that selectively bind to EphB receptors. The present invention also provides compositions, including pharmaceutical compositions, comprising the EphB receptor binding compounds and a pharmaceutically acceptable carrier or excipient. Methods for identifying compounds that selectively or specifically bind to a member of the EphB receptor family are also provided.06-17-2010
20100260673PHAGE DISPLAY PEPTIDE PROBES FOR IMAGING EARLY RESPONSES TO ANTIANGIOGENIC TREATMENT - Rapid assessment of cancer response to a therapeutic regimen can determine efficacy early in the course of treatment. Briefly described, embodiments of this disclosure, among others, encompass a class of molecular imaging probes that can predict tumor early responses to anti-angiogenic therapies, such as that based on Bevacizumab (AVASTIN™). In particular, the present disclosure provides peptides that selectively bind to vascularized taget tissues such as, but not limited to solid tumors, responsive to anti-angiogenic therapies and which can, therefore, be useful to selectively concentrate moieties such as detectable labels, or therapeutic agents, in a tumor. The detectable labels, therefore, provide a way to selectively detect and monitor tissues, and most advantageously tumors, that respond to anti-angiogenic therapies.10-14-2010
20120034164TRUNCATED CAR PEPTIDES AND METHODS AND COMPOSITIONS USING TRUNCATED CAR PEPTIDES - Disclosed are compositions and methods useful for targeting and internalizing molecules into cells of interest and for penetration by molecules of tissues of interest. The compositions and methods are based on peptide sequences, such as truncated CAR peptides, that are selectively internalized by a cell, penetrate tissue, or both. The disclosed internalization and tissue penetration is useful for delivering therapeutic and detectable agents to cells and tissues of interest.02-09-2012
20120034162Fullerene Assisted Cell Penetrating Peptides - A composition and method is described for intracellular delivery of fullerene containing peptides. The composition and method involve fullerene-substituted phenylalanine as part of a peptide based delivery system. The presence of a fullerene-substituted amino acid in a peptide is found to alter the intracellular transport properties of the peptide.02-09-2012
20100183511SMALL PEPTIDES SPECIFICALLY BIND TO COLORECTAL CANCERS - Cancers are extremely heterogeneous in terms of the frequency and types of mutations present in different malignant tumors. Thus, it is likely that uniform clinical treatment is not optimal for all patients, and that the development of individualized therapeutic regimens may be beneficial. Multiple, unique small peptides bind to cell lines derived from different colon adenocarcinomas. Within two hours of contact, the colorectal cancer cells are able to transfer a 07-22-2010
20100260672PEPTIDES THAT SPECIFICALLY BIND HGF RECEPTOR (CMET) AND USES THEREOF - A polypeptide or multimeric polypeptide construct having the ability to bind to cMet or a complex comprising cMet and HGF, and methods for use are disclosed.10-14-2010
20100189645METAL CHELATORS AND METHODS OF THEIR USE - Metal chelators of Formula I and Formula II are disclosed:07-29-2010
20100166654Single-Drug Multi-Ligand Conjugates for Targeted Drug Delivery - An adhesive is provided containing at least one synthetic polymer with receptor sites that enable the selective capture or release of a target molecule. A polymer is synthesized by polymerizing and cross-linking a functional monomer or functional copolymers in the presence of a target or template molecule allowing for reversible interactions between the polymer and the target molecule. The target molecule may be extracted from the polymer creating receptor sites complimentary to the target molecule. Alternatively, the target molecule may remain in the polymer network and be controllably released. The molecularly imprinted polymer is formulated into an adhesive. The adhesive can be used as a component in an in-vitro diagnostic device to release template molecules or to capture target molecules in vacated receptor sites in the synthetic polymer.07-01-2010
20110129418Brain Tumor Targeting Peptides and Methods - A method of diagnosing and treating a human glioblastoma multiforme (GBM) brain tumor in a subject is disclosed. The method includes administering to the subject, an effective amount of composition having a peptide 12-20 amino acid residues in length and selected for its ability to bind preferentially to a subtype of human GBM cells identified as brain tumor initiating cells (BTICs) or highly invasive glioma cells (HIGCs). Also disclosed are a phage-display screening method for identifying such therapeutic peptides, and peptides that hind specifically to BTICs or HIGCs.06-02-2011
20100183510EphB RECEPTOR-BINDING PEPTIDES - The application is related to the identification of peptides that selectively bind to Eph receptors of the B class. Also disclosed are uses of such peptides in the treatment of a variety of diseases. Additionally, imaging tumors in patients is described by administrating labeled peptides to patients and then obtaining an image of the labeled peptides.07-22-2010
20100226854MHC Peptide Complexes and Uses Thereof in Infectious Diseases - Novel compounds carrying ligands capable of binding to counter receptors on relevant target cells are disclosed. The compounds possess a number of advantageous features, rendering them very suitable for a wide range of applications, including use as detection systems, detection of relevant target cells as well as a number of other methods. In particular, novel MHC complexes comprising one or more MHC molecules are disclosed. The affinity and specificity of the MHC-peptide complexes are surprisingly high. The possibility of presenting to the target cells a plurality of MHC-peptide complexes makes the MHC complexes according to the present invention an extremely powerful tool e.g. in the field of therapy and diagnosis. The invention generally relates to the field of therapy, including therapeutic methods and therapeutic compositions. Also comprised by the present invention is the sample-mounted use of MHC complexes and MHC multimers.09-09-2010
20130216479SITE-SPECIFIC CHEMICAL MODIFICATION OF PROTEINS AT THEIR N-TERMINI, ENABLING THE FORMATION OF HOMOGENEOUS ADDUCTS - Site-specific modifications of proteins at their N-termini are provided. In particular, a chemical modification of proteins at their N-termini via a transamination reaction to form homogeneous adducts such as, the corresponding oxime derivatives is provided. Methods of making and using the adducts in radio-labelling, molecular imaging applications, and treatment of disorders such as cancer, Crohn's disease, arthritis, atherothrombosis and plaque rupture are also provided.08-22-2013
20100239497OXIDIZED AVIDIN WITH HIGH RESIDENCY TIME IN THE TREATED TISSUES - The present invention describes chemically modified avidins that have higher permanence in treated tissues compared to wild type avidin. Avidin oxidation is performed by periodate incubation in the presence of the low affinity ligand HABA which, occupying the biotin binding sites, prevents protein denaturation during the oxidation step. Periodate oxidation generates CHO groups from avidin mannose ring opening that, once injected, react with tissue NH09-23-2010
20120141377COMPOSITIONS AND METHODS FOR TREATING CANCER - A method of one or more of inhibiting motility, migration, dispersal, and metastasis of a cell that expresses an RPTP, which is proteolytically cleaved to form intracellular fragments in the cell includes administering to the cell an amount of an agent effective to inhibit one or more of the catalytic activity and function of the proteolytically cleaved intracellular domain-containing fragments of the RPTP.06-07-2012
20120141376PROSTATE SPECIFIC TRANSCRIPTS AND THE USE THEREOF FOR PROSTATE CANCER THERAPEUTICS AND DIAGNOSTICS - Genes that are up regulated in human prostate tumor tissues and the corresponding proteins are identified. These genes and the corresponding antigens are suitable targets for the treatment, diagnosis or prophylaxis of prostate cancer.06-07-2012
20090257951NGR receptor and methods of identifying tumor homing molecules that home to angiogenic vasculature using same - The present invention provides a method of identifying a tumor homing molecule that homes to angiogenic vasculature by contacting a substantially purified NGR receptor with one or more molecules and determining specific binding of a molecule to the NGR receptor, where the presence of specific binding identifies the molecule as a tumor homing molecule that homes to angiogenic vasculature. The invention also provides a method of directing a moiety to angiogenic vasculature in a subject by administering to the subject a conjugate including a moiety linked to a tumor homing molecule that exhibits specific binding to an NGR receptor, whereby the moiety is directed to angiogenic vasculature. In addition, the invention provides a method of imaging the angiogenic vasculature of a tumor in a subject by administering to the subject a conjugate having a detectable moiety linked to a tumor homing molecule that exhibits specific binding to an NGR receptor and detecting the conjugate.10-15-2009
20090074664CYCLIC AZAPEPTIDES AS INTEGRIN MARKERS - The present application is directed to radiolabeled cyclic polyazapeptides, pharmaceutical compositions comprising radiolabeled cyclic polyazapeptides, and methods of using the radiolabeled cyclic polyazapeptides. Such polyazapeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).03-19-2009
20110027177INHIBITION OF ANGIOGENESIS - The present invention is directed to novel methods of inhibiting angiogenesis using chlorotoxin agents. In some embodiments, the inventive methods include intravenous, intraocular, intravitreal, subjunctival injection, and/or topical administration of a chlorotoxin agent that may or may not be labeled. In some embodiments, the inventive methods allow treatment and/or amelioration of ocular diseases characterized by neovascularization, such as wet macular degeneration. In some embodiments, neovascularization is inhibited and/or newly formed vessels are caused to regress.02-03-2011
20090028788COMPOUNDS HAVING RD TARGETING MOTIFS - The present invention provides compounds that have motifs that target the compounds to cells that express integrins. In particular, the compounds have peptides with one or more RD motifs conjugated to an agent selected from an imaging agent and a targeting agent. The compounds may be used to detect, monitor and treat a variety of disorders mediated by integrins.01-29-2009
20110091380CHLOROTOXINS AS DRUG CARRIERS - The present invention relates to the use of a toxin moiety (e.g., a chlorotoxin moiety) as a carrier for therapeutic agents, e.g., therapeutic agents that require intracellular uptake to exert their effects. For example, in some embodiments, the present invention provides conjugates comprising a toxin (e.g., a chlorotoxin) moiety and an anti-cancer moiety and methods for using such conjugates to increase cellular uptake and/or increase specificity for cancer cells of the anti-cancer drug. In some embodiments, the present invention provides conjugates comprising a toxin moiety (e.g., a chlorotoxin moiety) and a nucleic acid agent. Also provided are methods of treatment involving administration of such conjugates, and pharmaceutical compositions and kits useful for carrying out such methods of treatment.04-21-2011
20090068102TREATING STROKE - Methods of treating stroke with blocking agents of TWEAK or TWEAK receptor are presented.03-12-2009
20110243845SOMATOSTATIN ANALOGS WITH INHIBITORY ACTIVITY TO GROWTH HORMONE RELEASE - Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.10-06-2011
20090092548Methods And Compounds For Targeting Tissues - The present invention relates to peptides which home to cells, e.g. heart cells, with high selectivity and which can be useful in the form of compositions. Such compositions can be used, e.g., for selectively targeting a systemically administered therapeutic agent or imaging agent to a cell or tissue in a subject. The present invention further relates to methods of using the compositions for imaging, e.g. PET imaging, and targeting cells, e.g. for delivering a therapeutic agent to one or more target cells in a subject.04-09-2009
20100034740RADIOFLUORINATION METHODS - The invention relates to conjugates of formula (V) or (VI), their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.02-11-2010
20090028790Labelled adrenomedullin derivatives and their use for imaging and therapy - The present invention relates to an adrenomedullin derivative including an adrenomedullin peptide, or a fragment thereof chelated or otherwise bound to at least one active agent. Examples of active agents include a paramagnetic element, a radioactive element and a fibrinolytic agent, among others. Paramagnetic agents have a distribution that is relatively easily shown through Magnetic Resonance Imaging (MRI). Radioactive agents have applications in imaging and delivery of radiations, depending on the specific element included in the active agent. Delivery of fibrinolytic agents mainly to a specific organ, such as for example to the lungs, allows to substantially improve the specificity and efficacy of thrombolytic therapy by allowing local delivery of the fibrinolytic agent, thereby reducing the risks of major bleeding in the therapy of the organ. If the organ is the lungs, a non-limiting example of pathology treatable with the fibrinolytic agent is pulmonary embolus.01-29-2009
20090028789Methods for detecting parenchymal plaques in vivo - Methods for detecting parenchymal plaque deposits in the brain of a living mammal are described that include administering a polyamine modified, labeled polypeptide having specific binding affinity for the extracellular deposit, to the living mammal. Isolated β-amyloid peptides that are polyamine modified and labeled with a radioisotope or contrast agent also are described.01-29-2009
20110176997METHOD TO MAKE POROUS MATERIALS AND THEIR APPLICATIONS - The present invention relates a method to make porous materials which are useful in pharmaceutical, medicine, industry, and agriculture. The most advantage of the porous materials is to provide extremely large surface area for further modification and to incorporate a bioactive reagent in a mild condition to make the porous materials bioactive, biocompatible and biodegradable.07-21-2011
20110150764STROKE-TAGETING PEPTIDE AND USE THEREOF - The present invention relates to stroke-targeting peptides and use thereof. More specifically, the present invention relates to a stroke-targeting peptide comprising an amino acid sequence selected from the group consisting of SEQ ID NO: 1 to SEQ ID NO: 4 and use thereof. The peptide of the present invention can be specifically bound to stroke cells in the subject, and thus can be effectively used in diagnostic markers and kits for stroke, and compositions for drug delivery specific to stroke and pharmaceutical compositions and compositions for imaging stroke.06-23-2011
20110097267COMPOSITIONS FOR IMAGING PAIN AND STRESS IN VIVO - Briefly described, embodiments of the present disclosure relate to methods and compositions for imaging pain and/or stress in a subject and methods and compositions for treating associated conditions. In particular, the present disclosure relates to the use of labeled compounds to provide objective diagnosis of pain and/or stress, for imaging regions associated with pain and/or stress, and for treating pain in a subject.04-28-2011
20120201753METHODS AND COMPOSITIONS RELATED TO TARGETING WOUNDS, REGENERATING TISSUE, AND TUMORS - Disclosed are compositions and methods useful for targeting regenerating tissue, wounds, and tumors. The compositions and methods are based on peptide sequences that selectively bind to and home to regenerating tissue, wound sites, and tumors in animals. The disclosed targeting is useful for delivering therapeutic and detectable agents to regenerating tissue, wound sites, and tumors in animals.08-09-2012
20100310455Heterocyclic Ligands for Integrin Imaging and Therapy - The present invention provides α12-09-2010
20110250133GASTRIN RELEASING PEPTIDE COMPOUNDS - Methods and compositions for diagnosing, staging disease, monitoring therapeutic effect of drugs and imaging a patient are provided, including radiopharmaceutical formulations. Compositions comprising Ga-AMBA complexed with a radioactive isotope are provided; as are methods of imaging Gastrin Releasing Peptide receptor (GRP-R) bearing tissue and methods of diagnosing or staging disease in patients suspected of having disease associated with aberrant GRP-R function. Further, methods of monitoring therapeutic effect of a drug targeted to a receptor that crosstalks with GRP-R are provided; as are methods of pre-dosing/co-dosing non-target tissues containing GRP-R. Particularly, methods of monitoring activity of receptors and receptor pathways in vivo/in vitro by using a ligand that binds to the GRP-R are provided; as are methods of measuring the activity of a receptor or group of receptors and their associated pathways that exhibit crosstalk with the GRP-R by using such a ligand which is also detectable by external means.10-13-2011
20090022664Radiolabelling via fluorination of aziridines - The present invention relates to novel compounds suitable for or already radiolabelled with 01-22-2009
20090324496Radioactive material for inhibiting cancer and preparation method thereof - A radioactive material for inhibiting cancer and a preparation method thereof are disclosed. The radioactive material for inhibiting cancer is M-SOCTA-Z and M is a radioactive nuclide such as 12-31-2009
20080286201Caspase-3 Substrate Comprising Imaging Agents - The present invention relates to diagnostic imaging agents for in vivo imaging. The imaging agents comprise a synthetic caspase-3 substrate peptide labelled with an imaging moiety suitable for diagnostic imaging in vivo. The invention also provides radiopharmaceutical compositions comprising the imaging agents, together with kits for the preparation of the radiopharmaceuticals. Also described are non-radioactive precursors suitable for the preparation of the imaging agents. The imaging agents are useful for the diagnostic imaging and or therapy monitoring in vivo of various disease states where caspase-3 is involved.11-20-2008
20080279772METHODS FOR DETECTING PATHOLOGICAL SITES - The present invention relates to the field of site directed therapy. More specifically the invention relates to site directed radio therapy, and provides a method for production of radioconjugates and an apparatus for radioimmunotherapy. The method, conjugates and apparatus can be practicalized without the need for radioactive shielding and/or airtight facilities. Without these restrictions the invention provides a simple and efficient means of therapy at the bed-side of the patient.11-13-2008
20080267867Metal Complexes of N-Heterocyclic Carbenes as Radiopharmaceuticals and Antibiotics - A method for inhibiting microbial growth comprises administering an effective amount of a silver complex of a N-heterocyclic amine. A method for treating cancer cells or a method for imaging one or more tissues of a patient includes administering an effective amount of a complex of a N-heterocyclic amine and a radioactive metal. N-heterocyclic carbenes of the present invention may be represented by formula (I) wherein Z is a heterocyclic group, and R10-30-2008
20110256057Cyclic Azapeptides as Integrin Markers and Methods of Using - The present application is directed to radiolabeled cyclic polyazapeptides, pharmaceutical compositions comprising radiolabeled cyclic polyazapeptides, and methods of using the radiolabeled cyclic polyazapeptides. Such polyazapeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).10-20-2011
20080219923Method and Kit for the Production of Particles Labelled with Rhenium-188 - Rhenium-188 labeled particles are produced by suspending particles of an organic polymer or a biopolymer in a solution wherein the solution contains a water-soluble tin-II salt and a Re-188 perrhenate salt with a radioactivity of 1,000 MBq to 60,000 MBq and wherein the solution has initially a pH value of pH 1 to pH 3; heating the solution of step a) to 80° C. to 100° C.; and, after 45 minutes to 70 minutes of heating, increasing and adjusting the pH value to a pH value of pH 5 to pH 8.5.09-11-2008
20110165075INTEGRIN TARGETING AGENTS AND IN-VIVO AND IN-VITRO IMAGING METHODS USING THE SAME - The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.07-07-2011
20110020224APPARATUS AND METHOD FOR PREPARING MEDICINES CONTAINING RADIOACTIVE SUBSTANCES - An apparatus (01-27-2011
20110020223POLYPEPTIDES HAVING AFFINITY FOR HER2 - HER2 binding polypeptides comprising the amino acid sequence EX01-27-2011
20110052491GASTRIN RELEASING PEPTIDE COMPOUNDS - New and improved compounds for use in diagnostic imaging or therapy having the formula M—N—O—P—G, wherein M is an optical label or a metal chelator (in the form complexed with a metal radionuclide or not), N—O—P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.03-03-2011
20100322857RADIOLABELLED PEPTIDE BASED COMPOUNDS AND USES THEREOF - The present invention relates to new radiolabelled peptide-based compounds and their use for diagnostic imaging using positron emission tomography (PET). Such compounds may thus be used for diagnosis or therapy of, for example, malignant diseases, heart diseases, endometriosis, inflammation-related diseases, rheumatoid arthritis and Kaposi's sarcoma.12-23-2010
20110097265QUANTIFICATION METHOD FOR REMAINING LIVER FUNCTION AND NOVEL LIVER RECEPTOR IMAGING AGENT - A test indicator for quantifying remaining liver function is provided. A novel liver receptor imaging agent with liver targeting property is utilized to develop a method for quantifying remaining liver function to serve as test indicator for judging the liver failure outcome in clinic, particularly for judging the necessity of liver transplantation for patients with liver failure or liver disease. The radioactivity uptake of the test indicator was negatively correlated with the extent of liver reserve. The cutoff value of liver reserve for liver transplantation is also disclosed.04-28-2011
20110097266Bombesin Analog Peptide Antagonist Conjugates - To provide a diagnostic and therapeutic medicament, a bombesin analog peptide antagonist conjugate is provided which has general Formula (I), wherein A is a metal chelator comprising at least one radionuclide metal, B is a spacer linked to N-terminal of C or a covalent bond and C is a bombesin analog peptide antagonist having a sequence as claimed, where further x is an integer from 1 to 3 and n is an integer from 1 to 6.04-28-2011
20110097264RADIOLABELING METHOD USING MULTIVALENT GLYCOLIGANDS AS HEPATIC RECEPTOR IMAGING AGENT - A radiolabeling method using a multivalent glycoligand as hepatic receptor imaging agent is provided. The multivalent glycoligand-DTPA derivatives (In-111-DTPA-hexa lactoside and In-111-DTPA-tri-galactosamine glycoside) labeled with In-111 are used as hepatic receptor imaging agent. The effects of imaging of a hepatic receptor in different species are evaluated, the lowest specific radioactivity values of hepatic receptor imaging required in different species are discovered. Since the specificity of the human ASGPR closely resembles that of the mouse. This kind of radiolabelling method, agent and related study about specific radioactivity could be used in clinical trial in the future.04-28-2011
20100158803Production and Use of Novel Peptide-Based Agents for Use with Bi-Specific Antibodies - The present invention relates to a bi-specific antibody or antibody fragment having at least one arm that is reactive against a targeted tissue and at least one other arm that is reactive against a targetable conjugate. The targetable conjugate encompasses a hapten to which antibodies have been prepared. In preferred embodiments, the hapten is histamine-succinyl-glycine (HSG). In more preferred embodiments, the at least one arm comprises the CDR sequences of the HSG-binding 679 antibody. The targetable conjugate is attached to one or more therapeutic and/or diagnostic agents. The invention provides constructs and methods for producing the bispecific antibodies or antibody fragments, as well as methods for using them and kits comprising them.06-24-2010
20100021381Natriuretic peptide-mediated imaging of atherosclerotic plaque - Tracers comprising an oligopeptide comprising a fragment of a natriuretic peptide, wherein the fragment comprises the sequence Arg-Ile-Asp-Arg-Ile (SEQ ID NO.: 1), and a signaling moiety, are disclosed. Further disclosed are methods of imaging atherosclerotic plaque by PET scanning or MRI using a tracer.01-28-2010
20120308481RADIO-OPAQUE COMPOUNDS, COMPOSITIONS CONTAINING SAME AND METHODS OF THEIR SYNTHESIS AND USE - Radio-opaque biodegradable compositions are formed by modifying terminal groups of synthetic and natural biodegradable polymers such as polylactones with iodinated moieties. The biodegradable property of the compositions renders them suitable for use in medical field such as drug delivery, imaging. Compounds disclosed in this invention exist as neat liquid. Certain compositions disclosed in this invention form hydrophobic iodine rich domains when dissolved in water, such domains provide better contrasting properties as well as ability to dissolve hydrophobic bioactive drugs. Certain iodinated moieties disclosed in the invention are capable of cross linking natural proteins in situ in presence of suitable catalysts and co-catalysts.12-06-2012
20110027176HOMING PEPTIDE FOR TUMOR VASCULATURE - This invention provides for a 9 mer peptide (CTPSPFSHC SEQ ID NO:1) that selectively binds to the tumor vasculature supporting tumors of the alimentary canal. The homing peptide has both diagnostic and therapeutic uses.02-03-2011
20090068103APTAMERS LABELED WITH 68GA - This invention relates to novel nucleotide-based compounds, methods of making radiolabeled compounds and use of such compounds for diagnostic imaging. Provided are compounds according to Formula (I) A-B-L-C, wherein A stands for an aptamer, B is absent or stands for a bridging structure, L is a linker, and C is a metal ion chelator. All substituents are defined in detail in the description. Preferred embodiments of said compounds bind to Tenascin-C.03-12-2009
20120039801SPARC binding peptides and uses thereof - Disclosed are SPARC and albumin binding peptides for the targeting of disease sites, such as tumors, with therapeutic and diagnostic agents In particular, compositions comprising SPARC binding peptide—Antibody Fc domain fusion proteins and methods of their use are disclosed.02-16-2012
20090280058Delivery Of Double-Stranded RNA Into The Central Nervous System - The present invention provides for compositions and methods for in vivo delivery of a cell-permeable complex to cells of the central nervous system, wherein the cell-permeable complex decreases the level of a functional target protein encoded by a target mRNA molecule. In preferred embodiments of the invention, the cell-permeable complex comprises an siRNA nucleic acid molecule operably linked to a cell-penetrating peptide, wherein the cell-penetrating peptide facilitates transport of the cell-permeable complex across both the blood brain barrier and cell membrane of a target cell. The methods of the invention further encompass the utilization of convection-enhanced delivery methods such as intracerebral clysis (ICC) to deliver the cell-permeable complex to the target cells of the central nervous system.11-12-2009
20110305634Methods and systems for adenovirus interaction with desmoglein 2 (DSG2) - The present invention provides compositions and methods for treating disorders associated with epithelial tissues.12-15-2011
20110305633Methods for Treatment, the Prognostic Assessment and the Detection of Breast Cancer - The present invention relates to methods for the treatment, the prognostic assessment and the detection of breast cancer.12-15-2011
20110110855NOVEL GHRELIN ANALOGUES - Ghrelin analogues having high affinity for a target receptor in diseased cells are provided, as well as methods of diagnosis and treatment utilizing such analogues.05-12-2011
20110110854Methods and Compositions for Improved F-18 Labeling of Proteins, Peptides and Other Molecules - The present application discloses compositions and methods of synthesis and use of 05-12-2011
20120039802PEPTIDES THAT SPECIFICALLY BIND HGF RECEPTOR (CMET) AND USES THEREOF - A polypeptide or multimeric polypeptide construct having the ability to bind to cMet or a complex comprising cMet and HGF, and methods for use are disclosed.02-16-2012
20110008251Methods for Generating Stably Linked Complexes Composed of Homodimers, Homotetramers or Dimers of Dimers and Uses - The present invention concerns methods and compositions for stably tethered structures of defined compositions, which may have multiple functionalities and/or binding specificities. Particular embodiments concern homodimers comprising monomers that contain a dimerization and docking domain attached to a precursor. The precursors may be virtually any molecule or structure, such as antibodies, antibody fragments, antibody analogs or mimetics, aptamers, binding peptides, fragments of binding proteins, known ligands for proteins or other molecules, enzymes, detectable labels or tags, therapeutic agents, toxins, pharmaceuticals, cytokines, interleukins, interferons, radioisotopes, proteins, peptides, peptide mimetics, polynucleotides, RNAi, oligosaccharides, natural or synthetic polymeric substances, nanoparticles, quantum dots, organic or inorganic compounds, etc. Other embodiments concern tetramers comprising a first and second homodimer, which may be identical or different. The disclosed methods and compositions provide a facile and general way to obtain homodimers, homotetramers and heterotetramers of virtually any functionality and/or binding specificity.01-13-2011
20110064658RGD-(bacterio)chlorophyll conjugates for photodynamic therapy and Imaging of Necrotic tumors - RGD-chlorophyll and RGD-bacteriochlorophyll conjugates that home and accumulate in necrotic tumor domains much longer than in tumor non-necrotic domains are provided for use in minimally invasive tumor-targeted imaging, tumor-targeted photodynamic therapy, and/or on-line prognosis of necrotic tumors.03-17-2011
20110064657LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), BIOLOGICAL EVALUATION, AND USE AS IMAGING AGENTS - The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.03-17-2011
20120045393LHRH-II PEPTIDE ANALOGS - The invention is directed to analogs of LHRH-II and, more generally, to analogs of the LHRH family in which modifications have been made that confer enhanced binding affinity for LHRH receptors and/or improved metabolic stability.02-23-2012
20120045394HUMAN AND MOUSE TARGETING PEPTIDES IDENTIFIED BY PHAGE DISPLAY - The present invention concerns methods and compositions for in vivo and in vitro targeting. A large number of targeting peptides directed towards human organs, tissues or cell types are disclosed. The peptides are of use for targeted delivery of therapeutic agents, including but not limited to gene therapy vectors. A novel class of gene therapy vectors is disclosed. Certain of the disclosed peptides have therapeutic use for inhibiting angiogenesis, inhibiting tumor growth, inducing apoptosis, inhibiting pregnancy or inducing weight loss. Methods of identifying novel targeting peptides in humans, as well as identifying endogenous receptor-ligand pairs are disclosed. Methods of identifying novel infectious agents that are causal for human disease states are also disclosed. A novel mechanism for inducing apoptosis is further disclosed.02-23-2012
20120064003COMPLEX FOLATE-NOTA-Ga68 - The present invention concerns a Ga68 complex of formula FOLATE-(LINKER)i-NOTA-Ga03-15-2012
20110033380COMPOUNDS AND METHODS FOR USE IN DIAGNOSING AND TREATING MELANOMA, INCLUDING METASTATIC MELANOMA AND METHODS RELATED TO SAME - The present invention is directed to novel non-invasive diagnostic tools/compounds comprising a cyclic peptide wherein the compound binds to a MSH receptor to image and treat cancers, especially, melanoma, including metastatic melanoma in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probes are capable of detecting cancerous melanoma cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention will also be useful to initiate therapy for melanoma as well as monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.02-10-2011
20120207676NEUROTENSIN ANALOGUES FOR RADIOISOTOPE TARGETING TO NEUROTENSIN RECEPTOR-POSITIVE TUMORS - The invention relates to a new neurotensin analogue, or a salt thereof, useful for targeting to neurotensin receptor-positive tumors, like ductal pancreatic adenocarcinoma, exocrine pancreatic cancer, invasive ductal breast cancers, colon adeno-carcinoma, small cell lung carcinoma, Ewing sarcoma, meningioma, medulloblastoma and astrocytoma.08-16-2012
20120207675Method of Colorectal Cancer Detection by Using Radiolabeled Anti-GRP78 Peptide - The present disclosure describes techniques used for colorectal cancer detection. Position and distribution of colorectal cancer tumor are detected through nuclear imaging. Alternatively, stage of colorectal cancer is identified by shading value in tumor. Thus, the present disclosure provides a safe and noninvasive clinical method for diagnosing and tracing level and distribution of colorectal cancer before and after treatment.08-16-2012
20120128587FOLATE-TARGETED DIAGNOSTICS AND TREATMENT - Methods of detecting and assessing functionally active folate receptors on tumors and treatment associated with those tumors are described. Also described are methods of selecting ovarian and lung cancer patients for therapy with a folate-vinca conjugate by identifying functionally active folate receptors on the tumors of the patient. Also described are methods and compositions for treating folate receptor expressing epithelial tumors with a folate-vinca conjugate in combination with doxorubicin such as pegylated liposomal doxorubicin in which the tumors include ovarian, endometrial or non-small cell lung cancer tumors, including platinum-resistant ovarian tumors and platinum sensitive ovarian tumors. Also described are methods of treating platinum-resistant ovarian cancer using a folate-targeted drug, in the absence or presence of selecting the patient by identifying functionally active folate receptors on the tumors of the patient.05-24-2012
20120009123Albumin binding peptide-mediated disease targeting - The invention provides compositions and methods for delivering a therapeutic or diagnostic agent to a disease site in a mammal, the method comprising administering to the mammal a therapeutically or diagnostically effective amount of a pharmaceutical composition, wherein the pharmaceutical composition comprises the therapeutic or diagnostic agent coupled to an albumin binding peptide and a pharmaceutically acceptable carrier.01-12-2012
20120009124USE OF BUFFERS FOR RADIONUCLIDE COMPLEXATION - The present invention relates to a method for complexation of a chelate with a radionuclide, advantageously gallium, the complexation being carried out advantageously at ambient temperature without heating, by adding the radionuclide to the chelate in a buffer solution, the buffer of this solution comprising between two and five functions for coordination with the radionuclide, each coordination function being independently chosen from a carboxylic acid function and a hydroxyl function, on the condition that the buffer comprises at least one carboxylic acid function and at most two carboxylic acid functions. It also relates to the injectable solution obtained.01-12-2012
20120009122GASTRIN RELEASING PEPTIDE COMPOUNDS - New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure:01-12-2012
20120301397DIAGNOSIS OF MACROPHAGE MEDIATED DISEASE - The invention relates to a method of treating or monitoring/diagnosing a disease state mediated by activated macrophages. The method comprises the step of administering to a patient suffering from a macrophage mediated disease state an effective amount of a composition comprising a conjugate or complex of the general formula11-29-2012
20120014873PEPTIDES WHOSE UPTAKE BY CELLS IS CONTROLLABLE - A generic structure for the peptides of the present invention includes A-X-B-C, where C is a cargo moiety, the B portion includes basic amino acids, X is a cleavable linker sequence, and the A portion includes acidic amino acids. The intact structure is not significantly taken up by cells; however, upon extracellular cleavage of X, the B-C portion is taken up, delivering the cargo to targeted cells. Cargo may be, for example, a contrast agent for diagnostic imaging, a chemotherapeutic drug, or a radiation-sensitizer for therapy. X may be cleaved extracellularly or intracellularly. The molecules of the present invention may be linear, cyclic, branched, or have a mixed structure.01-19-2012
20120156132TARGETING AGENT TO NEWLY FORMED BLOOD VESSELS - It is an object of the present invention to provide a targeting agent that enables drug delivery to a neovascular site and the imaging of such a neovascular site, utilizing the effect of the agent to accumulate in the neovascular site. The present invention provides a targeting agent to a neovascular site, which comprises a gelatin-like protein.06-21-2012
20080317668Integrin Targeted Synthetic Ligands for Diagnostic and Therapeutic Applications - The present invention relates to a novel class of diagnostically or therapeutically effective compounds comprising novel aza-bicycloalkane based cyclic peptides, acting as a targeting moiety towards integrin receptors.12-25-2008
20080305041Pf4 Pharmacophores and Their Uses - The invention provides a novel PF4 pharmacophore that is useful, inter alia, for identifying peptidomimetics and other compounds capable of modulating PF4 activity (e.g., as inhibitors, agonists or antagonists). Mutant PF4 polypeptide sequences are also provided that modulate PF4 activity in cells.12-11-2008
20090246132Monoclonal antibodies (MAbs) against tumor-associated antigens, the preparation and use thereof - The invention relates to murine monoclonal antibodies (MAbs), A, B, C and D, which are directed against tumor-associated antigens. The nearly complete nucleotide sequences of the V genes of these MAbs are described, so that the relevant variable domains can be put together to give chimeric MAbs, or “humanized” MAbs are obtained by inserting the hypervariable regions (complementarity determining regions=CDR) into a human MAb framework. Antibody constructs of this type can be employed in human therapy and in vivo diagnosis without the disadvantages observed with murine MAbs.10-01-2009
20100290987METHODS AND COMPOSITIONS FOR DETECTING AND MODULATING O-GLYCOSYLATION - The invention relates to methods and products for modulating glycosylation of proteins. The invention is useful for identifying therapeutic compounds to treat glycosylation-associated disorders such as neurodegeneration, diabetes, including complications of diabetes such as insulin resistance, nephropathy, microvascular damage, and endothelial dysfunction. The invention is also useful for identifying therapeutic compounds to treat de-glycosylation-associated disorders such as ischemic damage and traumatic injury. The invention also relates in part to assays that are useful for identifying and testing candidate compounds for modulating glycosylation of proteins and also relates in part to compounds to treat glycosylation-associated diseases and disorders.11-18-2010
20120121507PEPTIDE LIGANDS FOR CLUSTERIN AND USES THEREOF - Peptides are disclosed that are useful for molecular imaging or diagnosis of a disease state, such as cancer, in which clusterin is upregulated.05-17-2012
20080260639PREPARATION AND METHOD UTILIZING RADIOLABELED CHLOROTOXIN - The inventors propose to label a chlorotoxin with I-123 or I-124 for a diagnostic agent, and with I-124 or I-131 for a therapeutic agent to reduce tumors and then to use a process they previously invented to stabilize the radiopharmaceutical. The inventors propose to reconstitute the preferred agents and administer them cyclically to diagnose and treat tumors. The inventors also propose a TETA or DOTA link to a metal radioisotope.10-23-2008
20100129290SMART CONTRAST AGENT AND DETECTION METHOD FOR DETECTING TRANSITION METAL IONS - The present disclosure provides smart contrast agents for transition metals and a method of using the same. The smart contrast agents include a core peptide and a first labeling group attached to a first end of the core peptide. The smart contrast agents can also include a second labeling group attached to a second end of the core peptide. The core peptide can bind to transition metals, and can be homologous to a fragment selected from the extended octarepeat region of a prion protein.05-27-2010
20120164072NANO-SIZED PARTICLES COMPRISING MULTI-HEADED AMPHIPHILES FOR TARGETED DRUG DELIVERY - Nano-sized particles are provided comprising at least one multi-headed amphiphilic compound, in which at least one headgroup of said multi-headed amphiphilic compound is selectively cleavable or contains a selectively cleavable group, and at least one biologically active agent, which is both encapsulated within the nano-particle and non-covalently associated thereto.06-28-2012
20120164071Compositions and Methods Comprising Phosphatidylethanolamine-Binding Peptide Derivatives - Disclosed are surprising discoveries concerning the role of anionic phospholipids and aminophospholipids in tumor vasculature and in viral entry and spread, and compositions and methods for utilizing these findings in the treatment of cancer and viral infections. Also disclosed are advantageous antibody, immunoconjugate and duramycin-based compositions and combinations that bind and inhibit anionic phospholipids and aminophospholipids, for use in the safe and effective treatment of cancer, viral infections and related diseases.06-28-2012
20100247434Anti-Angiogenic Extracts from Pomegranate - An extract of Chinese blackberry (09-30-2010
20110182811NUCLEOTIDE SEQUENCE ENCODING A MODULATOR OF NF-KB - The present invention relates to nucleotide sequences encoding a modulator of NF-κB, and to the polypeptides encoded by the nucleotide sequences. In particular, the invention relates to nucleotide sequences and the polypeptides encoded thereby, wherein the polypeptides are involved in the response to NF-κB-activating stimuli, including HTLV-1 Tax, LPS, PMA and IL-1. The invention also relates to antibodies to the modulator of NF-κB, methods of detecting modulator of NF-κB using the antibodies, methods of treatment associated with NF-κB activation and to methods of identifying compounds which modulate the activity of the modulator of NF-κB.07-28-2011
20120134923RADIOIODINATION METHOD - The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are novel radioiodinated BTMs prepared using the method, as well as radiopharmaceutical compositions comprising such radioiodinated BTMs. The invention also provides radioiodinated intermediates useful in the method, as well as in vivo imaging methods using.05-31-2012
20120219499COMPOSITIONS AND METHODS FOR DETECTING PLECTIN-1 AS A BIOMARKER FOR CANCER - The present invention provides compositions and methods useful for diagnostic and imaging techniques for detecting and localizing the biomarker Plectin-1. The present invention provides multimeric peptide ligand complexes for targeting Plectin-1, such as the multimeric peptide ligand complex having the formula (βAKTLLPTPGGS(PEG5000))4 KKKKDOTAβA-NH08-30-2012
20120219498COMPOSITIONS AND METHODS FOR INDUCING ANGIOGENESIS - An isolated peptide comprising an amino acid sequence HWRR as set forth by SEQ ID NO:5, the peptide consists of 4 or 5 amino acids, is provided. Also provided are methods of treating angiogenesis-related pathologies using the peptide of the invention or pharmaceutical compositions comprising same.08-30-2012
20120134922PEPTIDES WHOSE UPTAKE IN CELLS IS CONTROLLABLE - Disclosed herein, in certain embodiments, is a selective transport molecule with increased in vivo circulation. In some embodiments, a selective transport molecule disclosed herein has the formula (A—X—B—C)n—M, wherein C is a cargo moiety; A is a peptide with a sequence comprising 5 to 9 consecutive acidic amino acids, wherein the amino acids are selected from: aspartates and glutamates; B is a peptide with a sequence comprising 5 to 20 consecutive basic amino acids; X is a linker; and M is a macromolecular carrier.05-31-2012
20100172835METHODS AND COMPOSITIONS FOR SYNAPHICALLY-TARGETED TREATMENT FOR CANCER - Disclosed are compositions and methods useful for targeting therapeutics to cancerous cells and tumors. The disclosed targeting is useful for delivering therapeutic and detectable agents to cancerous cells and tumors.07-08-2010
20120251445PEPTIDES WHOSE UPTAKE BY CELLS IS CONTROLLABLE - A generic structure for the peptides of the present invention includes A-X-B-C, where C is a cargo moiety, the B portion includes basic amino acids, X is a cleavable linker sequence, and the A portion includes acidic amino acids. The intact structure is not significantly taken up by cells; however, upon extracellular cleavage of X, the B-C portion is taken up, delivering the cargo to targeted cells. Cargo may be, for example, a contrast agent for diagnostic imaging, a chemotherapeutic drug, or a radiation-sensitizer for therapy. Cleavage of X allows separation of A from B, unmasking the normal ability of the basic amino acids in B to drag cargo C into cells near the cleavage event. X is cleaved extracellularly, preferably under physiological conditions. D-amino acids are preferred for the A and B portions, to minimize immunogenicity and nonspecific cleavage by background peptidases or proteases.10-04-2012
20120171117RADIOFLUORINATED COMPOUNDS AND THEIR PREPARATION - The present invention provides a process for [07-05-2012
20120251446Peptide Conjugates Comprising Polyhistidine Sequence and Free Cysteine and Their Uses in Imaging - Bioconjugates for use in imaging are disclosed include a linker sequence fused to a polypeptide capable of binding a target in a biological system. The linker sequence is designed so that it is capable of being radiolabelled, e.g. with a complex comprising a radionuclide, via a free cysteine residue and the polyhistidine sequence in the label that are both capable of simultaneously binding to a complex comprising the radionuclide. These interactions can improve significantly the rate and efficiency of radiolabelling compared to either protein with the His-tag or the free cysteine alone. Optionally, the free cysteine residue provides a site which can be covalently bonded to a moiety such as a second label, in a site-specific manner.10-04-2012
20120251444TREATMENT OF LIVER DISORDERS BY ADMINISTRATION OF RAP CONJUGATES - The present invention relates to the use of receptor-associate protein (RAP) and fragments and variants thereof to improve delivery of therapeutic compounds to the liver and provides methods to treat liver disorders and conditions, such as hepatic carcinoma, by administering RAP or RAP variants conjugated to active agents.10-04-2012
20120076728HUMAN PROTEIN SCAFFOLD WITH CONTROLLED SERUM PHARMACOKINETICS - This invention provides constructs comprising a protein scaffold, wherein the scaffold comprises Domain III, Domain IIIa, or Domain IIIb of human serum albumin or a polypeptide having substantial sequence identity to the Domain III, the Domain IIIa, or the Domain IIIb; and a targeting moiety in covalent linkage to the protein scaffold; and a therapeutic moiety and/or an imaging moiety in covalent linkage to the protein scaffold. The scaffold can be modified to tune the serum pharmacokinetics of the construct. In addition to methods of making the constructs, therapeutic, imaging and diagnostic uses of the constructs are also provided.03-29-2012
20100047169NK Cell Receptor Conjugates for Treating Malignancies - The present invention relates generally to compositions useful in therapies involving the selective destruction of tumor cells in vivo. In particular, this invention relates to a conjugate which comprises a target recognition segment and an active cytotoxic segment. The target recognition segment comprises a receptor specific to NK cells, wherein the receptor binds to a cellular ligand expressed on the surface of a tumor cell, and the active segment comprises an agent capable of exerting a cytotoxic effect on the tumor cell. The target recognition segment derived form the natural killer receptor NKp30 has been found to be particularly effective in vivo.02-25-2010
20100047168Soluble Zcytor 11 Cytokine Receptors - Novel polypeptide combinations, polynucleotides encoding the polypeptides, and related compositions and methods are disclosed for soluble zcytor11 receptors that may be used as novel cytokine antagonists, and within methods for detecting ligands that stimulate the proliferation and/or development of hematopoietic, lymphoid and myeloid cells in vitro and in vivo. Ligand-binding receptor polypeptides and antibodies can also be used to block TIF activity in vitro and in vivo, and may be used in conjunction with TIF and other cytokines to selectively stimulate the immune system. The present invention also includes methods for producing the protein, uses therefor and antibodies thereto.02-25-2010
20120177571PANCREATIC ENDOCRINE CELL INDICATING AGENT AND UTILIZATION OF SAME - A pancreatic endocrine cell indicating agent of the present invention includes a modified polypeptide in which a metal chelator binds only to an amino acid that is located at a site other than a somatostatin receptor-binding active site in a polypeptide selected from the group consisting of somatostatin and somatostatin analogs; and a radioactive metal nuclide held by the metal chelator. According to the present invention, it is therefore possible to provide a novel pancreatic endocrine cell indicating agent.07-12-2012
20100272644COMPLEXATION OF FATTY ACID-CONJUGATED MOLECULES WITH ALBUMIN - The technology described herein is directed to conjugating various therapeutic or functional molecules, such small chemical drugs, peptides, oligonucleotides, isotopes and imaging regents with fatty acids, such as LCFAs. The fatty acid-conjugated molecules are complexed with a human serum albumin protein in vitro.10-28-2010
20100272643Procaspase 8-Mediated Disease Targeting - The invention provides compositions and method for delivering a therapeutic or diagnostic agent to a disease site in a mammal, the method comprising administering to the mammal a therapeutically or diagnostically effective amount of a pharmaceutical composition, wherein the pharmaceutical composition comprises the therapeutic or diagnostic agent coupled to a Procaspase 8 polypeptide and a pharmaceutically acceptable carrier.10-28-2010
20100008855Production and Use of Novel Peptide-Based Agents with Bispecific Antibodies - The present invention relates to a bi-specific antibody or antibody fragment having at least one arm that specifically binds a targeted tissue and at least one other arm that specifically binds a targetable construct. The targetable construct comprises a carrier portion which comprises or bears at least one epitope recognizable by at least one arm of said bi-specific antibody or antibody fragment. The targetable construct further comprises one or more therapeutic or diagnostic agents or enzymes. The invention provides constructs and methods for producing the bi-specific antibodies or antibody fragments, as well as methods for using them.01-14-2010
20090074663Peptide for diagnosing, preventing and treating atherosclerosis and uses thereof - A peptide for diagnosing, preventing and treating atherosclerosis, and a use thereof, comprising an amino acid sequence as set forth in SEQ ID NO: 1 or SEQ ID NO: 2, and a use thereof. The peptide effectively targets atherosclerotic plaques, and binds to IL-4R to thereby exhibit antagonistic effects on IL-4-mediated signaling of cellular inflammatory reaction and survival reaction. The peptide of the present invention can be used for diagnosis of atherosclerosis, prevention and treatment of IL-4-induced inflammatory reaction and prevention and treatment of atherosclerosis which is primarily caused by the inflammatory reaction, as well as for prevention or treatment of atherosclerosis via conjugation with an anti-atherosclerotic drug.03-19-2009
20120237444IODINE RADIOLABELLING METHOD - The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are novel radioiodinated BTMs prepared using the method, as well as radiopharmaceutical compositions comprising such radioiodinated BTMs. The invention also provides radioiodinated intermediates useful in the method, as well as in vivo imaging methods using the radioiodinated BTMs.09-20-2012
20120082619Labelled adrenomedullin derivatives and their use for imaging and therapy - The present invention relates to an adrenomedullin derivative including an adrenomedullin peptide, or a fragment thereof chelated or otherwise bound to at least one active agent. Examples of active agents include a paramagnetic element, a radioactive element and a fibrinolytic agent, among others. Paramagnetic agents have a distribution that is relatively easily shown through Magnetic Resonance Imaging (MRI). Radioactive agents have applications in imaging and delivery of radiations, depending on the specific element included in the active agent. Delivery of fibrinolytic agents mainly to a specific organ, such as for example to the lungs, allows to substantially improve the specificity and efficacy of thrombolytic therapy by allowing local delivery of the fibrinolytic agent, thereby reducing the risks of major bleeding in the therapy of the organ. If the organ is the lungs, a non-limiting example of pathology treatable with the fibrinolytic agent is pulmonary embolus.04-05-2012
20090016957Polypeptides - This invention relates to polypeptides which bind to EGFR family receptors and to applications of those polypeptides in medicine, veterinary medicine, diagnosis diagnostics and imaging.01-15-2009
20080299040SOMATOSTATIN RECEPTOR 2 ANTAGONISTS - The invention is directed to somatostatin analogs which are receptor antagonists of the somatostatin receptor, including receptor-selective antagonists, especially sst2-selective antagonists. Related compounds and compositions are included, including antagonists complexed with or conjugated to radioactive nuclides. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases; such methods, and kits, are encompassed.12-04-2008
20080299039Aprotinin Polypeptides for Transporting a Compound Across the Blood-Brain Barrier - The invention relates to improvements in the field of drug delivery. More particularly, the invention relates to polypeptides derived from aprotinin and from aprotinin analogs as well as conjugates and pharmaceutical compositions comprising these polypeptides or conjugates. The present invention also relates to the use of these polypeptide for transporting a compound or drug across the blood-brain barrier of a mammal and in the treatment and diagnosis of neurological diseases.12-04-2008
20110002848MOLECULES THAT SELECTIVELY HOME TO VASCULATURE OF PRE-MALIGNANT DYSPLASTIC LESIONS OR MALIGNANCIES - The present invention provides a conjugate that contains a therapeutic moiety linked to a homing peptide or peptidomimetic which selectively homes to vasculature of pre-malignant dysplastic skin and which includes the amino acid sequence SRPRR (SEQ ID NO: 1) or a conservative variant or peptidomimetic thereof. The present invention further provides a conjugate containing a therapeutic moiety linked to a homing peptide or peptidomimetic which selectively homes to vasculature of malignant skin and which includes the amino acid sequence CGKRK (SEQ ID NO: 6) or the amino acid sequence CDTRL (SEQ ID NO: 7), or a conservative variant or peptidomimetic of one of these sequences.01-06-2011
20120263645RADIOLABELED COMPOUND DIRECTABLE IN VIVO TO TARGET TISSUE AND USE THEREOF - The present invention provides a clinically usable radiolabeled compound that is precisely directable in vivo to a target tissue. The compound of the present invention has a first polypeptide or an analogue thereof, and a second polypeptide bonded to an N-terminus of the first polypeptide or the analogue thereof. In the compound, the first polypeptide is a polypeptide that specifically binds with a protein expressed in a target tissue, the second polypeptide has an amino acid region that has a high affinity for a radioactive metal nuclide, and the radioactive metal nuclide that has a high affinity for the amino acid region is held in the amino acid region.10-18-2012
20110229409LINKABLE LEWIS X ANALOGS - Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLe09-22-2011
20110236310LABELING COMPOSITION FOR INTRAOCULAR TISSUE, LABELING METHOD OF INTRAOCULAR TISSUE, AND SCREENING METHOD - The invention provides a labeling composition for an intraocular tissue of a living individual, which specifically labels the intraocular tissue without need of an invasive operation such as exposure of an ocular tissue or injection of a staining agent into the ocular tissue or a nerve tissue linking to the ocular tissue, a method of noninvasively labeling an intraocular tissue of a living individual, and a screening method using the labeling composition for the intraocular tissues. The composition contains a compound capable of labeling at least a photoreceptor cell layer of a retina, wherein the compound is a staining compound having a particular structure as a partial structure thereof.09-29-2011
20110236309ANTAGONISTS OF LIGANDS AND USES THEREOF - The invention provides hetero-multivalent ligand binging agents (traps) for members of the TGF-β superfamily, as well as methods for making and using such constructs. In an embodiment of the invention there is provided a hetero-multivalent binding agent with affinity for a member of the TGF-β superfamily, said agent comprising the general structure (I): (-linker1)09-29-2011
2010023308268GA-Labeled Peptide-Based Radiopharmaceuticals - The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise targeting vectors which bind to integrin receptors.09-16-2010
2009022041999mTc-LABELED TRIPHENYLPHOSPHONIUM DERIVATIVE CONTRASTING AGENTS AND MOLECULAR PROBES FOR EARLY DETECTION AND IMAGING OF BREAST TUMORS - Tc-labeled triphenylphosphonium contrasting agents that target the mitochondria and are useful for early detection of breast tumors using scintimammographic imaging. 09-03-2009
20120328516METHOD OF RADIOTHERAPY USING A RADIOLABELLED RGD PEPTIDE - The present invention relates to a method of radiotherapy, in particular image-guided radiotherapy (IGRT), where radiolabelled RGD peptides are used to provide a tumour angiogenesis volume. Also provided are methods of determination of the gross tumour volume as well as methods of radiotherapy monitoring using such peptides.12-27-2012
20120328517KALLIKREIN-BINDING "KUNITZ DOMAIN" PROTEINS AND ANALOGUES THEREOF - This invention provides: novel protein homologous of a Kunitz domain, which are capable of binding kallikrein; polynucleotides that encode such novel proteins; and vectors and transformed host cells containing these polynucleotides.12-27-2012
20120328515IN VIVO DETECTION OF APOPTOSIS - The invention provides methods and products, such as kits, useful for determining the apoptotic state of cells in an organism.12-27-2012
20100215577COMPOSITIONS AND METHODS FOR VISUALIZING AND ELIMINATING CANCER STEM CELLS - The present invention relates generally to the field of cancer diagnosis and treatment, and more particularly to compositions and methods that may be useful for eliminating cancer cells with stem-like characteristics. The disclosed compositions and methods may also be useful for managing breast cancer, ovarian cancer, cervical cancer or endometrial (uterine) cancer with metastases; and visualizing the cancer cells in patient's body. The compositions of the instant invention include human prolactin receptor antagonist G129R.08-26-2010
20100215576DIAGNOSIS AND TREATMENT OF NEUROECTODERMAL TUMORS - The present invention provides fusion proteins for the detection and treatment of neuroectodermal tumors. Previous work demonstrated that chlorotoxin is specific for glial-derived or meningioma-derived tumor cells. The current invention has extended the use of chlorotoxin-cytotoxin fusion proteins to treat the whole class neuroectodermal tumors such as gliomas, meningiomas, ependymonas, medulloblastomas, neuroblastomas, gangliomas, pheochromocytomas, melanomas, PPNET's, small cell carcinoma of the lung, Ewing's sarcoma, and metastatic tumors in the brain. Also, diagnostic methods are provided for screening neoplastic neuroectodermal tumors.08-26-2010
20120100072PET IMAGING OF FIBROGENESIS - The present invention relates to peptide compounds and their use for in vivo imaging using positron emission tomography (PET). More specifically, the invention relates to the use of such peptide-based compounds in a method for the in vivo imaging of liver fibrosis.04-26-2012
20120100071SYNTHESIS AND USE OF RADIOLABELLED INSULIN ANALOGUES - A radiolabelled insulin analogue is provided. The analogue comprises a radiolabel linked to an insulin analogue at an amino acid at the terminal end of the B chain of the insulin analogue.04-26-2012
20120100070Cyclic Peptide Analogues For Non-Invasive Imaging of Pancreatic Beta-Cells - Compositions, methods of using and methods of making a cyclic peptide analog imaging agent that includes at least portions of a peptide or protein that binds specifically to the GLP-1 receptor (GLP-1R) and the cyclic analog has one or more conformational restrictions including, but not limited to, lactam bridges, disulfide bridges, hydrocarbon bridges, and their combinations, salts and derivatives thereof wherein the cyclic analog is more stable than a non-cyclic analog when incubated in the presence of enzymes that degrade GLP-1 and have an increased serum half-live, wherein the cyclic analog comprises at least a portion of a GLP-1 peptide or at least a portion of an Exendin peptide salts, derivatives or combinations thereof.04-26-2012
20120288442Nuclear Imaging Method Using Molecular Target Detection Agent for Liver Fibrosis - A method for diagnosing liver fibrosis is provided. A monoclonal antibody and an antagonist of cannabinoid receptor in liver fibrosis cell are labeled. The monoclonal antibody or the antagonist is injected for nuclear imaging. Thus, through the image obtained through the nuclear imaging, liver fibrosis is diagnosed and traced in clinic use for preventive medicine.11-15-2012
20100202964Organ Homing Genes of Cancer Metastases - Provided herein are methods that use liver targeting domains of colon cancer, such as for example PA28alpha, HNRNPA1, and/or KIAA1407, and the polynucleotides that encode them, for the prognosis, diagnosis, detection, staging and/or prediction of survival rates in individuals with colon cancer, whether the cancer has metastasized or not, as well as for imaging purposes and design of diagnostic and/or therapeutic methods.08-12-2010
20100034739Fungus-Specific Imaging Agents - The disclosure relates to an imaging composition including a fungus-specific peptide and an imaging material. Another imaging composition includes a fungus-specific peptide and a chelator able to chelate a radionuclide. The disclosure also provides to a method of detecting a fungal infection. The method includes administering an imaging agent to a patient. The imaging agent comprises a fungus-specific peptide and an imaging material. Then one may detect the imaging agent in the patient. Detecting retained imaging agent in a tissue or organ indicates fungal infection of the tissue or organ.02-11-2010
20090257952Engineered Integrin Binding Peptides - Engineered peptides that bind with high affinity (low equilibrium dissociation constant (Kd)) to the cell surface receptors of fibronectin (α10-15-2009
20130011335Materials and Methods Related to Sodium/Potassium Adenosine Triphosphate and SRC - This invention is based in part on the elucidation of new structural conformations and functions of the sodium/potassium adenosine triphosphate synthase (Na/K ATPase), and especially elucidation of new binding sites and interactions. The present invention provides practical applications of several surprising structural and functional relationships between Na/K ATPase and compounds which interact with Na/K ATPase. Disclosure of these structures and relationships provides insight and practical solutions to chemically affecting not only the Na/K ATPase interactions, but also regulators known to be upstream and downstream.01-10-2013
20130011334MODIFIED UBIQUITIN PROTEINS HAVING A SPECIFIC BINDING ACTIVITY FOR THE EXTRADOMAIN B OF FIBRONECTIN - The present invention refers to novel hetero-multimeric proteins obtained from modified ubiquitin capable of binding the extradomain B of fibronectin (ED-B) with high affinity. Furthermore, the invention refers to fusion proteins comprising said recombinant protein fused to a pharmaceutically and/or diagnostically active component. The invention is further directed to the use of said proteins in medical treatment methods.01-10-2013
20080247946Gastrin Releasing Peptide Compounds - New and improved compounds for use in radiodiagnostic imaging or radiotherapy having the formula M-N—O—P-G, wherein M is the metal chelator (in the form complexed with a metal radionuclide or not), N—O—P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and/or providing radiotherapy to a patient using the compounds of the invention are also provided. A method for preparing a diagnostic imaging agent from the compound is further provided. A method for preparing a radiotherapeutic agent is further provided.10-09-2008
20080226551Transport Molecules Using Reverse Sequence HIV-TAT Polypeptides - This invention relates to novel transport molecules that comprise a polypeptide comprising amino acid residues arranged in a sequence that is the reverse-sequence of basic portion of the HIV-TAT protein. The novel transport polypeptides are useful for transmembrane or intracellular delivery of cargo molecules, non-limiting examples of which include polypeptides and nucleic acids. The novel transport polypeptides may be covalently or non-covalently bound to the cargo modules.09-18-2008
20110262353MUTEINS OF HNGAL AND RELATED PROTEINS WITH AFFINITY FOR A GIVEN TARGET - The present invention relates to novel muteins derived from human lipocalin 2 (hNGAL) and related proteins that bind a given non-natural ligand with detectable affinity. The invention also relates to corresponding nucleic acid molecules encoding such a mutein and to a method for their generation. The invention further relates a method for producing such a mutein. Furthermore, the invention is directed to a pharmaceutical composition comprising such a lipocalin mutein as well as to various uses of the mutein.10-27-2011
20130171068HEPATOCYTE GROWTH FACTOR FRAGMENTS THAT FUNCTION AS POTENT MET RECEPTOR AGONISTS AND ANTAGONISTS - The NK1 fragment of hepatocyte growth factor (HGF) binds to and activates the Met receptor, a transmembrane receptor tyrosine kinase that plays a critical role in embryonic development and organ formation. The instant application discloses NK1 variant polypeptides which act as agonists or antagonists of HGF. Further disclosed are covalently linked NK1 variant polypeptides. Many of the disclosed variant polypeptides possess improved stability characteristics.07-04-2013
20130171069NEUROTOXIC TARGET FOR AMYLOSPHEROID, METHOD AND MATERIAL FOR REDUCING THE NEUROTOXICITY OF AMYLOSPHEROID, AND USE THEREOF - In one or a plurality of embodiments, there is provided a target molecule of amylospheroid, which is expressed in mature neurons and to which the amylospheroid binds to induce death of cells. Further, in one or a plurality of embodiments, there is provided a method and a substance for inhibiting death of mature neurons induced by the amylospheroid. In one aspect, the present disclosure relates to a use of Na07-04-2013
20110274619BRAIN TUMOR TARGETING PEPTIDES AND METHODS - A method of diagnosing and treating a human glioblastoma multiforme (GBM) brain tumor in a subject is disclosed. The method includes administering to the subject, an effective amount of composition having a peptide 12-20 amino acid residues in length and selected for its ability to bind preferentially to a subtype of human GBM cells identified as brain tumor initiating cells (BTICs) or highly invasive glioma cells (HIGCs).11-10-2011
20110274618DIAGNOSTIC AND/OR THERAPEUTIC AGENT, METHOD FOR THE MANUFACTURE THEREOF AND USE THEREOF - The invention relates to the fields of materials sciences and medicine and relates to an agent, which can be used, for example, as a contrast medium for the localization of cancer cells. The object of the present invention is to disclose an agent which sensitively and selectively recognizes the site and the type of the molecules or cells to be examined. The object is attained through an agent composed at least of bio-shuttle molecules to which endohedral fullerenes are coupled by way of peptide-based molecules, wherein the endohedral fullerenes are hydrophobic and correspond to the formula A11-10-2011
20120093724METHODS AND COMPOSITIONS FOR THE DETECTION OF CANCER - Various embodiments of this invention relate generally to targeted activation and delivery of therapeutic drugs to cells that produce prostate specific antigen (PSA), prostate specific membrane antigen (PSMA) or human glandular kallikrein (hK2). Various further embodiments relate more specifically to PSMA-specific peptide prodrugs that become activated to yield therapeutic drugs. Further aspects of various embodiments of the present invention also relate to methods and compositions for treating or preventing cancers and methods and compositions for detecting and/or imaging cancers.04-19-2012
20120093723NANOCARRIER COMPOSITIONS AND METHODS - This invention provides multimeric nanocarrier for in vivo delivery of a bioactive agent, comprising at least two peptide monomers reversibly or irreversibly linked with one or more of said bioactive agents, wherein said two or more of said peptide monomers are covalently linked by a biodegradable difunctional moiety, as well as methods of using this nanocarrier.04-19-2012
20120093722SYNTHETIC DIBLOCK COPOLYPEPTIDE HYDROGELS FOR USE IN THE CENTRAL NERVOUS SYSTEM - This invention relates, e.g., to a composition suitable for administration to the central nervous system (CNS), comprising a block copolypeptide hydrogel, which comprises a biologically active material that is mixed with the hydrogel or that is attached to the polypeptide chain of the hydrogel, wherein the composition is suitable for administration to the CNS. Also disclosed are methods of making and using compositions of the invention as depots or as scaffolds for cell migration, and pharmaceutical compositions and kits for implementing methods of the invention.04-19-2012
20120093721USES OF CANCER-TARGETING PEPTIDES IN CANCER DIAGNOSIS - Cancer-targeting peptides and uses thereof in cancer diagnosis.04-19-2012
20080213175Click chemistry-derived cyclic peptidomimetics as integrin markers - The present application is directed to radiolabeled cyclic peptidomimetics, pharmaceutical compositions comprising radiolabeled cyclic peptidomimetics, and methods of using the radiolabeled cyclic peptidomimetics. Such peptidomimetics can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).09-04-2008
20130136692MOLECULAR SIGNATURE OF CANCER - The present invention provides compounds, compositions, and methods for detecting, diagnosing and treating cancers such as glioblastoma multiforme.05-30-2013
20130115167PEPTIDES THAT HOME TO ATHEROSCLEROTIC PLAQUES AND METHODS OF USE - The invention provides methods of targeting atherosclerotic plaques using LyP-1 related peptides. The invention additionally provides methods of treating an inflammatory condition using LyP-1 related peptides.05-09-2013
20130095036METHODS AND COMPOSITIONS FOR DIAGNOSIS OF IGA-AND IGM-MEDIATED KIDNEY DISEASES - The present invention features noninvasive methods for diagnosing IgA or IgM kidney disorders, such as IgA nephropathy, Henoch-Schönlein purpura, and IgM nephropathy, in a mammal. The invention also features compositions and kits useful in diagnosing these disorders.04-18-2013
20130095037PEPTIDE DERIVATIVES OF EXENDIN-4 - In the current invention peptides, which are derived from GLP-1 (glucagon-like peptide-1) and exendin-3 and/or exendin-4, are provided which bond to the GLP-1 receptor and can be used, labeled or unlabeled, for the production of an agent for diagnostic and therapy of benign and malignant diseases, in which GLP-1 receptor expression plays a role.04-18-2013
20130129623RADIOPHARMACEUTICAL COMPOSITIONS - The present invention relates to 05-23-2013
20130129622CYCLOPENTAPEPTIDE DERIVATIVES AND USES THEREOF - The present invention, among others, relates to a compound having a structure according to formula (I) or a pharmaceutically acceptable salt thereof, wherein Xaa05-23-2013
20130129621Integrin Receptor Antagonists and Their Methods of Use - Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH05-23-2013
20130136691GASTRIN RELEASING PEPTIDE COMPOUNDS - Methods and compositions for diagnosing, staging disease, monitoring therapeutic effect of drugs and imaging a patient are provided, including radiopharmaceutical formulations. Compositions comprising Ga-AMBA complexed with a radioactive isotope are provided; as are methods of imaging Gastrin Releasing Peptide receptor (GRP-R) bearing tissue and methods of diagnosing or staging disease in patients suspected of having disease associated with aberrant GRP-R function. Further, methods of monitoring therapeutic effect of a drug targeted to a receptor that crosstalks with GRP-R are provided; as are methods of pre-dosing/co-dosing non-target tissues containing GRP-R. Particularly, methods of monitoring activity of receptors and receptor pathways in vivo/in vitro by using a ligand that binds to the GRP-R are provided; as are methods of measuring the activity of a receptor or group of receptors and their associated pathways that exhibit crosstalk with the GRP-R by using such a ligand which is also detectable by external means.05-30-2013
20080199397Use of a Tetrapeptide Acsdkp Analogue Resistant to the Angiotensin i Conversion Enzyme, for Measuring Glomerular Filtration Rate in a Human or an Animal and Kit Containing Same - The invention concerns the use of ACE-resistant N-acetyl-Ser-Asp-Lys-Pro analogues for preparing a reagent or marker adapted to measure a glomerular filtration rate.08-21-2008
20110236311RADIOLABELLING METHODS - The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II):09-29-2011
20130149241PEPTIDE RADIOTRACER COMPOSITIONS - The present invention relates to imaging agent compositions comprising radiolabelled c-Met binding peptides suitable for positron emission tomography (PET) imaging in vivo. The c-Met binding peptides are labelled with the radioisotope 06-13-2013
2013014924099mTc-LABELED TRIPHENYLPHOSPHONIUM DERIVATIVE CONTRASTING AGENTS AND MOLECULAR PROBES FOR EARLY DETECTION AND IMAGING OF BREAST TUMORS - 99mTc-labeled triphenylphosphonium contrasting agents that target the mitochondria and are useful for early detection of breast tumors using scintimammographic imaging. 99mTc-Mito10-MAG3 possesses advantageous radiopharmaceutical properties. The uptake in the myocardium is reduced by one to two orders of magnitude compared to 99mTc-MIBI. 99mTc-Mito10-MAG3 exhibits fast blood clearance, with a blood half-life of less than 2 minutes in rats. A diminished myocardial uptake combined with a prompt reduction of cardiovascular blood pool signal to facilitate improved signal-to-background ratios.06-13-2013
201301492395-PYRROLIDINYLSULFONYL-ISATIN DERIVATIVES - The present invention relates to novel 06-13-2013
20130156696HUMAN ANTIBODIES AGAINST PSEUDOMONAS AERUGINOSA LPS DERIVED FROM TRANSGENIC XENOMOUSE - The invention described herein provides for human antibodies produced in non-human animals that specifically bind to 06-20-2013
20130156697ISOLATED PROTEIN MEDICAMENT - The invention in suitable embodiments is directed to an isolated protein comprising one or more amino acid sequences, each amino acid sequence capable of being functionalized and/or attached in whole and/or in part to one or more or a plurality of elements of one or more types including to cargo elements, forming a composition of elements suitable for use as an in vivo and/or in vitro medicament to treat one or more biological species.06-20-2013
20130183237THROMBIN INHIBITOR - The invention relates to thrombin inhibitors derived from the salivary glands of haematophagous arthropods and in particular to bivalent and trivalent thrombin inhibitors that act by interacting with thrombin at two or three different sites.07-18-2013
20110311446PEPTIDES THAT SPECIFICALLY BIND HGF RECEPTOR (CMET) AND USES THEREOF - A polypeptide or multimeric polypeptide construct having the ability to bind to cMet or a complex comprising cMet and HGF, and methods for use are disclosed.12-22-2011
20110311445DIAGNOSIS AND TREATMENT OF MYELOID AND LYMPHOID CELL CANCERS - Disclosed is a method of diagnosing and treating myeloproliferative or lymphoproliferative cell disorders, such as cancer, with chlorotoxin and/or derivatives, analogs or fragments thereof, which are effective to bind to an inhibit abnormal myeloid or lymphoid cell growth.12-22-2011
20130189186APOPTOSIS IMAGING AGENTS BASED ON LANTIBIOTIC PEPTIDES - The present invention relates to radiopharmaceutical imaging in vivo of apoptosis. The invention provides imaging agents which target apoptotic cells via selective binding to the aminophospholipid phosphatidylethanolamine (PE), which is exposed on the surface of apoptotic cells. The radiopharmaceuticals comprise radiometal complexes of chelator conjugates of PE-binding peptides. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.07-25-2013
20120003152COMPOSITIONS AND METHODS OF USE OF TARGETING PEPTIDES FOR DIAGNOSIS AND THERAPY OF HUMAN CANCER - The present invention concerns compositions comprising and methods of identification and use of targeting peptides selective for cancer tissue, particularly prostate or ovarian cancer tissue. The method may comprise identifying endogenous mimeotopes of such peptides, such as GRP78, IL-11Rα and hsp90. Antibodies against such targeting peptides or their mimeotopes may be used for detection, diagnosis and/or staging of prostate or ovarian cancer. In other embodiments, the compositions and methods concern a novel type of gene therapy vector, known as adeno-associated phage (AAP). AAP are of use for targeted delivery of therapeutic agents to particular tissues, organs or cell types, such as prostate or ovarian cancer. In still other embodiments, targeting peptides selective for low-grade lipomas may be used for detection, diagnosis and targeted delivery of therapeutic agents.01-05-2012
20120020882PEPTIDE-BASED COMPOUNDS - The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise targeting vectors which bind to integrin receptors.01-26-2012
20120020881Triaryl-sulphonium compounds, kit and methods for labeling positron emitting isotopes - This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 01-26-2012
20120034163NON-INVASIVE TOOLS FOR DETECTING VULNERABLE ATHEROSCLEROTIC PLAQUES - The present invention relates to a polypeptide comprising the sequence RILAR (SEQ ID NO: 3), the use thereof in imaging methods, in diagnostic or prognostic methods and for use as a medicament.02-09-2012
20090004104Methods and Compositions for Delivering Active Agents with Enhanced Pharmacological Properties - Provided herein are methods of enhancing in vivo efficacy of an active agent, comprising: administering to a subject an active agent that is coupled to a bioelastic polymer or elastin-like peptide, wherein the in vivo efficacy of the active agent is enhanced as compared to the same active agent when administered to the subject not coupled to (or not associated with) a bioelastic polymer or ELP.01-01-2009
20090180952Ligands binding the complex of urokinase-type plasminogen activator (uppa) and its receptor (upar) that inhibit downstream upar interactions: identification and use in diagnosis or therapy - Antibodies or other ligands specific for the binary uPA-uPAR complexes, for ternary complexes comprising uPA-uPAR and for complexes of uPAR and proteins other than uPA such as integrins inhibit the interaction of uPA and uPAR with additional molecules with which the complexed interact. Such antibodies or other ligands are used in diagnostic and therapeutic methods, particularly against cancer.07-16-2009
20080279771Novel Imaging Agents for Cancer - A novel imaging agent is described which comprises a semaphorin moiety and an imaging moiety. The novel imaging agent of the invention may be used in the diagnostic imaging of cancer and in particular, for targeting angiogenesis or metaplasia. Further aspects of the present invention presented herein include a method for the preparation of the imaging agent, a pharmaceutical composition comprising the imaging agent of the invention and a kit for the preparation of said pharmaceutical.11-13-2008
20130209358RADIOTRACER COMPOSITIONS - The present invention relates to [08-15-2013
20130209359Small Peptides Specifically Bind to Colorectal Cancers - Cancers are extremely heterogeneous in terms of the frequency and types of mutations present in different malignant tumors. Thus, it is likely that uniform clinical treatment is not optimal for all patients, and that the development of individualized therapeutic regimens may be beneficial. Multiple, unique small peptides bind to cell lines derived from different colon adenocarcinomas. Within two hours of contact, the colorectal cancer cells are able to transfer a 08-15-2013

Patent applications in class Attached to peptide or protein of 2+ amino acid units (e.g., dipeptide, folate, fibrinogen, transferrin, sp. enzymes); derivative thereof