P38a MAP kinase

Pyridinyl imidazoles have been used as fluorescent reporters of binding to p38a MAP kinase.12,13 To measure kon for test compounds, the kinase was... 

Dynamics in the p38a MAP kinase-SB203580 complex observed by liquid-state NMR spectroscopy. Angewandte Chemie - International Edition in English, 47, 3548-3551. 

Profiling the structural determinants of heteroarylnitrile scaffold-based derivatives as falcipain-2 inhibitors by in silico methods 13CMD2032. Recent developments of p38a MAP kinase inhibitors as antiinflammatory agents based on the imidazole scaflblds 13CMD1997. 

Design, synthesis and bioiogicai activity of a novel series of naphthyridinone derivatives as potent p38a MAP kinase inhibitors for the treatment of rheumatoid arthritis... 

Gill AL, frederickson M, Cleasby A, Woodhead SJ, Carr MG, Woodhead AJ, Walker MT, Congreve MS, Devine LA, Tisi D, O Reilly M, Seavers LCA, Davis DJ, Curry J, Anthony R, Padova A, Murray CW, Carr RAE, Jhoti H (2005) Identification of novel p38a MAP kinase inhibitors using fragment-based lead generation. J Med Chem 48 414-426... 

Perry JJP, Harris RM, Moiani D, Olson AJ, Tainer JA (2009) p38a MAP kinase C-terminal domain binding pocket characterized by crystallographic and computational analyses. J Mol Biol 391 1-11... 

Fig. 7 List of positive compounds and a representative merged image. Sampie protein His-p38a MAP kinase. The iisted compound SB203580, an inhibitor of p38a MAP kinase, is indicated by a redcoior on the image arrows)...

KC706 Inhibitor enzyme conformation MAP kinase p38a Inflammatory diseases Phase II... 

The assignments for two protein kinases have been recently published for active murine PKA [33] and for the inactive human MAP kinase p38a [47]. Both kinases have been studied by numerous other biophysical methods and... 

Tumor necrosis factor alpha (TNFa) and interleukin-1 beta (IL-1(3) are proinflammatory cytokines implicated in many inflammatory diseases such as rheumatoid arthritis (RA), inflammatory bowel disease, and psoriasis. P38a is a mitogen activated protein (MAP) kinase that plays an essential role in the signal transduction pathways leading to the synthesis of TNFa and IL-1(3. Thus, inhibition of p38 MAP kinase has remained a popular drug development target for orally active small molecules. 

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