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1nvs

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{{STRUCTURE_1nvs| PDB=1nvs | SCENE= }}
{{STRUCTURE_1nvs| PDB=1nvs | SCENE= }}
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'''The Complex Structure Of Checkpoint Kinase Chk1/SB218078'''
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===The Complex Structure Of Checkpoint Kinase Chk1/SB218078===
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==Overview==
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Chk1 is a serine-threonine kinase that plays an important role in the DNA damage response, including G(2)/M cell cycle control. UCN-01 (7-hydroxystaurosporine), currently in clinical trials, has recently been shown to be a potent Chk1 inhibitor that abrogates the G(2)/M checkpoint induced by DNA-damaging agents. To understand the structural basis of Chk1 inhibition by UCN-01, we determined the crystal structure of the Chk1 kinase domain in complex with UCN-01. Chk1 structures with staurosporine and its analog SB-218078 were also determined. All three compounds bind in the ATP-binding pocket of Chk1, producing only slight changes in the protein conformation. Selectivity of UCN-01 toward Chk1 over cyclin-dependent kinases can be explained by the presence of a hydroxyl group in the lactam moiety interacting with the ATP-binding pocket. Hydrophobic interactions and hydrogen-bonding interactions were observed in the structures between UCN-01 and the Chk1 kinase domain. The high structural complementarity of these interactions is consistent with the potency and selectivity of UCN-01.
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{{ABSTRACT_PUBMED_12244092}}
==About this Structure==
==About this Structure==
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[[Category: Zhou, B B.]]
[[Category: Zhou, B B.]]
[[Category: Chk1-sb218078 complex]]
[[Category: Chk1-sb218078 complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 03:02:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 00:48:01 2008''

Revision as of 21:48, 27 July 2008

Image:1nvs.png

Template:STRUCTURE 1nvs

The Complex Structure Of Checkpoint Kinase Chk1/SB218078

Template:ABSTRACT PUBMED 12244092

About this Structure

1NVS is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural basis for Chk1 inhibition by UCN-01., Zhao B, Bower MJ, McDevitt PJ, Zhao H, Davis ST, Johanson KO, Green SM, Concha NO, Zhou BB, J Biol Chem. 2002 Nov 29;277(48):46609-15. Epub 2002 Sep 19. PMID:12244092

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