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2p3g
From Proteopedia
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[[Image:2p3g.jpg|left|200px]] | [[Image:2p3g.jpg|left|200px]] | ||
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'''Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2''' | '''Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2''' | ||
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[[Category: Caspers, N.]] | [[Category: Caspers, N.]] | ||
[[Category: Kurumbail, R G.]] | [[Category: Kurumbail, R G.]] | ||
| - | [[Category: | + | [[Category: Atp-binding]] |
| - | [[Category: | + | [[Category: Kinase domain]] |
| - | [[Category: | + | [[Category: Map kinase]] |
| - | [[Category: | + | [[Category: Mk-2]] |
| - | [[Category: | + | [[Category: Mk2]] |
| - | [[Category: | + | [[Category: Serine/threonine kinase]] |
| - | [[Category: | + | [[Category: Transferase]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 12:16:04 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 09:16, 4 May 2008
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. 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 Sun May 4 12:16:04 2008
