1yqj

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Image:1yqj.gif

1yqj, resolution 2.00Å

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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 with SO4 and 6NP as ligands. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 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

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