RhoB can adopt a Mg2+ free conformation prior to GEF binding.
|Author||Soundararajan, Meera; Turnbull, Andrew; Fedorov, Oleg; et al|
|Subject||Enzyme Stability Guanine Nucleotide Exchange Factors Hydrolysis Magnesium Models, Molecular Protein Binding Protein Structure, Secondary rhoA GTP-Binding Protein rhoB GTP-Binding Protein drug effects metabolism drug effects metabolism pharmacology drug effects chemistry chemistry metabolism|
SH2 domains: modulators of nonreceptor tyrosine kinase activity.
|Abstract||The Src homology 2 (SH2) domain is a sequence-specific phosphotyrosine-binding module present in many signaling molecules. In cytoplasmic tyrosine kinases, the SH2 domain is located N-terminally to the catalytic kinase domain (SH1) where it mediates cellular localization, substrate recruitment, and regulation of kinase activity. Initially, structural studies established a role of the SH2 domain stabilizing the inactive state of Src family members ... [truncated at 450 characters in length]|
|Author||Filippakopoulos, Panagis; Müller, Susanne; Knapp, Stefan;|
|Subject||Disease Enzyme Activation Enzyme Stability Humans Mutation Protein-Tyrosine Kinases src Homology Domains genetics chemistry genetics metabolism|
New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights.
|Abstract||Protein kinase casein kinase 2 (CK2) is a serine/threonine kinase with evidence of implication in growth dysregulation and apoptosis resistance, making it a relevant target for cancer therapy. Several CK2 inhibitors have been developed showing variable efficiency, emphasizing the need to expand the chemical diversity of those inhibitors. We report the identification and characterization of 2,8-difurandicarboxylic acid derivatives as a new class o ... [truncated at 450 characters in length]|
|Author||López-Ramos, Miriam; Prudent, Renaud; Moucadel, Virginie; et al|
|Subject||Animals Binding Sites Casein Kinase II Cell Line, Tumor Crystallography, X-Ray Enzyme Activation Enzyme Inhibitors Enzyme Stability Humans Proto-Oncogene Proteins c-pim-1 antagonists and inhibitors chemistry drug effects chemical synthesis chemistry pharmacology antagonists and inhibitors chemistry|