1nvq
From Proteopedia
(New page: 200px<br /> <applet load="1nvq" size="450" color="white" frame="true" align="right" spinBox="true" caption="1nvq, resolution 2.0Å" /> '''The Complex Structur...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:1nvq. | + | [[Image:1nvq.jpg|left|200px]]<br /><applet load="1nvq" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1nvq" size=" | + | |
caption="1nvq, resolution 2.0Å" /> | caption="1nvq, resolution 2.0Å" /> | ||
'''The Complex Structure Of Checkpoint Kinase Chk1/UCN-01'''<br /> | '''The Complex Structure Of Checkpoint Kinase Chk1/UCN-01'''<br /> | ||
| Line 8: | Line 7: | ||
==About this Structure== | ==About this Structure== | ||
| - | 1NVQ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 and UCN as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1NVQ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=UCN:'>UCN</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1NVQ OCA]. |
==Reference== | ==Reference== | ||
| Line 27: | Line 26: | ||
[[Category: chk1-ucn-01 complex]] | [[Category: chk1-ucn-01 complex]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:31:07 2008'' |
Revision as of 14:31, 15 February 2008
|
The Complex Structure Of Checkpoint Kinase Chk1/UCN-01
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
1NVQ is a Single protein structure of sequence from Homo sapiens with and as ligands. 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 Fri Feb 15 16:31:07 2008
Categories: Homo sapiens | Single protein | Bower, M.J. | Concha, N.O. | Davis, S.T. | Green, S.M. | Johanson, K.O. | McDevitt, P.J. | Zhao, B. | Zhao, H. | Zhou, B.B. | SO4 | UCN | Chk1-ucn-01 complex
