2p3g
From Proteopedia
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Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2
Overview
A new class of potent kinase inhibitors selective for mitogen-activated, protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) for the, treatment of rheumatoid arthritis has been prepared and evaluated. These, inhibitors have IC50 values as low as 10 nM against the target and have, good selectivity profiles against a number of kinases including CDK2, ERK, JNK, and p38. These MK-2 inhibitors have been shown to suppress TNFalpha, production in U397 cells and to be efficacious in an acute inflammation, model. The structure-activity relationships of this series, the, selectivity for MK-2 and their activity in both in vitro and in vivo, models are discussed. The observed selectivity is discussed with the aid, of an MK-2/inhibitor crystal structure.
About this Structure
2P3G is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.
Reference
Pyrrolopyridine Inhibitors of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK-2)., Anderson DR, Meyers MJ, Vernier WF, Mahoney MW, Kurumbail RG, Caspers N, Poda GI, Schindler JF, Reitz DB, Mourey RJ, J Med Chem. 2007 May 31;50(11):2647-54. Epub 2007 May 5. PMID:17480064
Page seeded by OCA on Wed Jan 23 14:55:39 2008
