Regulator of G-protein signaling 14 (RGS14) is a selective H-Ras effector.
|Abstract||Regulator of G-protein signaling (RGS) proteins have been well-described as accelerators of Galpha-mediated GTP hydrolysis ("GTPase-accelerating proteins" or GAPs). However, RGS proteins with complex domain architectures are now known to regulate much more than Galpha GTPase activity. RGS14 contains tandem Ras-binding domains that have been reported to bind to Rap- but not Ras GTPases in vitro, leading to the suggestion that RGS14 is a Rap-specif ... [truncated at 450 characters in length]|
|Author||Willard, Francis S; Willard, Melinda D; Kimple, Adam J; et al|
|Subject||Animals Binding Sites Cell Differentiation Extracellular Signal-Regulated MAP Kinases Fibroblast Growth Factor 2 Humans Mice Mitogen-Activated Protein Kinases Multiprotein Complexes Nerve Growth Factor Neurites PC12 Cells Protein Binding RGS Proteins Rats raf Kinases ras Proteins antagonists and inhibitors physiology antagonists and inhibitors physiology physiology metabolism|
Selective inhibition of BET bromodomains.
|Abstract||Epigenetic proteins are intently pursued targets in ligand discovery. So far, successful efforts have been limited to chromatin modifying enzymes, or so-called epigenetic 'writers' and 'erasers'. Potent inhibitors of histone binding modules have not yet been described. Here we report a cell-permeable small molecule (JQ1) that binds competitively to acetyl-lysine recognition motifs, or bromodomains. High potency and specificity towards a subset of ... [truncated at 450 characters in length]|
|Author||Filippakopoulos, Panagis; Qi, Jun; Picaud, Sarah; et al|
|Subject||Amino Acid Sequence Animals Azirines Binding Sites Carcinoma, Squamous Cell Cell Differentiation Cell Line, Tumor Cell Proliferation Chromatin Dihydropyridines Female Humans Mice Mice, Nude Models, Molecular Molecular Sequence Data Nuclear Proteins Protein Binding Protein Structure, Tertiary Recombinant Proteins Sequence Alignment Skin Neoplasms Stereoisomerism Transcription Factors chemical synthesis chemistry pharmacology physiopathology drug effects drug effects metabolism chemical synthesis chemistry pharmacology antagonists and inhibitors metabolism drug effects metabolism physiopathology antagonists and inhibitors metabolism|