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2p3g

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{{STRUCTURE_2p3g| PDB=2p3g | SCENE= }}
{{STRUCTURE_2p3g| PDB=2p3g | SCENE= }}
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'''Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2'''
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===Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 17480064 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17480064}}
==About this Structure==
==About this Structure==
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[[Category: Serine/threonine kinase]]
[[Category: Serine/threonine kinase]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 12:16:04 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 13:04:16 2008''

Revision as of 10:04, 28 July 2008

Image:2p3g.png

Template:STRUCTURE 2p3g

Crystal structure of a pyrrolopyridine inhibitor bound to MAPKAP Kinase-2

Template:ABSTRACT PUBMED 17480064

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

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