Patent application number | Description | Published |
20090062150 | COMPOSITIONS AND METHODS FOR REGULATING INTRAMEMBRANE PROTEASES - Structural models for a rhomboid protease alone and bound to inhibitors and peptide substrates and compositions and methods for preparing rhomboid protease binding compounds and methods for using such rhomboid protease binding compounds for modulation of these proteases catalytic activity are disclosed herein. | 03-05-2009 |
20090239244 | MODULATORS OF PROTEIN PHOSPHATASE 2A AND PP2A METHYL ESTERASE - The disclosure relates to modulation of protein phosphorylation, including information derived from the structures and activities of the proteins designated protein phosphatase 2A (PP2A) and PP2A methyl esterase. The disclosure contained herein provides compounds and methods for identification of compounds that antagonize the function of PME, and thus reduce levels of PP2A demethylation activity. Over-expression or gain-of-function of PME contributes to a range of diseases such as cancer, thus inhibition of PME by antagonists may provide a strategy for therapeutic intervention. | 09-24-2009 |
20090274682 | DEMETHYLATION AND INACTIVATION OF PROTEIN PHOSPHATASE 2A - Embodiments of the present invention relate to atomic coordinates for PME-1 alone or in complex with PP2A, as well as methods for using these atomic coordinates to prepare inhibitors of PME-1 and/or PP2A and inhibitors prepared using such methods. Further embodiments relate to biochemical analyses of the interactions of PME-1 alone or in complex with PP2A. Further embodiments relate to compositions including mimetics and small molecules, optionally, secondary agents, which may be used to treat disorders in which PME-1 and/or PP2A activity plays a contributing role. | 11-05-2009 |
20090291878 | MODULATORS OF PROTEIN PHOSPHATASE 2A HOLOENYME - Atomic coordinates for human serine/threonine protein phosphotase 2A (PP2A) holoenzyme, as well as methods for using these atomic coordinates to prepare inhibitors of PP2A and inhibitors prepared using such methods are provided herein. A biochemical analysis of the interactions of PP2A holoenzyme is also provided. Compositions including mimetics and small molecules of the invention and, optionally, secondary agents may be used to treat disorders in which PP2A activity plays a contributing role. | 11-26-2009 |
20100092480 | MODULATORS OF PROTEIN PHOSPHATASE 2A - Atomic coordinates for human serine/threonine protein phosphotase 2A (PP2A) core, as well as methods for using these atomic coordinates to prepare inhibitors of PP2A and inhibitors prepared using such methods are provided herein. A biochemical analysis of the interactions of PP2A core is also provided. Compositions including mimetics and small molecules of the invention and, optionally, secondary agents may be used to treat disorders in which PP2A activity plays a contributing role. | 04-15-2010 |
20100261914 | IAP BINDING COMPOUNDS - Compounds that bind cellular IAPs (inhibitor of apoptosis proteins) are disclosed. The compounds are mimetics of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABOLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these compounds for therapeutic, diagnostic and assay purposes. | 10-14-2010 |