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1nvs

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{{Structure
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|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UCM:REL-(9R,12S)-9,10,11,12-TETRAHYDRO-9,12-EPOXY-1H-DIINDOLO[1,2,3-FG&#58;3&#39;,2&#39;,1&#39;-KL]PYRROLO[3,4-I][1,6]BENZODIAZOCINE-1,3(2H)-DIONE'>UCM</scene>
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|RELATEDENTRY=[[1nvq|1nvq]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1nvs FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1nvs OCA], [http://www.ebi.ac.uk/pdbsum/1nvs PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1nvs RCSB]</span>
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'''The Complex Structure Of Checkpoint Kinase Chk1/SB218078'''
'''The Complex Structure Of Checkpoint Kinase Chk1/SB218078'''
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[[Category: Zhao, H.]]
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[[Category: Zhou, B B.]]
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[[Category: chk1-sb218078 complex]]
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[[Category: Chk1-sb218078 complex]]
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Revision as of 00:02, 3 May 2008

Image:1nvs.jpg

Template:STRUCTURE 1nvs

The Complex Structure Of Checkpoint Kinase Chk1/SB218078


Overview

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.

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 Page seeded by OCA on Sat May 3 03:02:26 2008

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