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1yqj
From Proteopedia
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| , resolution 2.00Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , | ||||||
| Gene: | MAPK14, CSBP, CSBP1, CSBP2, MXI2 (Homo sapiens) | ||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal Structure of p38 Alpha in Complex with a Selective Pyridazine Inhibitor
Overview
Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition of LPS-induced TNF-alpha production in mice and exhibited good efficacy in the rat collagen induced arthritis model.
About this Structure
1YQJ is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase., Tamayo N, Liao L, Goldberg M, Powers D, Tudor YY, Yu V, Wong LM, Henkle B, Middleton S, Syed R, Harvey T, Jang G, Hungate R, Dominguez C, Bioorg Med Chem Lett. 2005 May 2;15(9):2409-13. PMID:15837335
Page seeded by OCA on Mon Mar 31 01:18:22 2008
