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1q0b
From Proteopedia
(New page: 200px<br /> <applet load="1q0b" size="450" color="white" frame="true" align="right" spinBox="true" caption="1q0b, resolution 1.9Å" /> '''Crystal structure of...) |
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| - | [[Image:1q0b.gif|left|200px]]<br /> | + | [[Image:1q0b.gif|left|200px]]<br /><applet load="1q0b" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1q0b" size=" | + | |
caption="1q0b, resolution 1.9Å" /> | caption="1q0b, resolution 1.9Å" /> | ||
'''Crystal structure of the motor protein KSP in complex with ADP and monastrol'''<br /> | '''Crystal structure of the motor protein KSP in complex with ADP and monastrol'''<br /> | ||
==Overview== | ==Overview== | ||
| - | We report here the first inhibitor-bound structure of a mitotic motor | + | We report here the first inhibitor-bound structure of a mitotic motor protein. The 1.9 A resolution structure of the motor domain of KSP, bound with the small molecule monastrol and Mg2+ x ADP, reveals that monastrol confers inhibition by "induced-fitting" onto the protein some 12 A away from the catalytic center of the enzyme, resulting in the creation of a previously non-existing binding pocket. The structure provides new insights into the biochemical and mechanical mechanisms of the mitotic motor domain. Inhibition of KSP provides a novel mechanism to arrest mitotic spindle formation, a target of several approved and investigative anti-cancer agents. The structural information gleaned from this novel pocket offers a new angle for the design of anti-mitotic agents. |
==About this Structure== | ==About this Structure== | ||
| - | 1Q0B 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 MG, ADP and NAT as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1Q0B 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=MG:'>MG</scene>, <scene name='pdbligand=ADP:'>ADP</scene> and <scene name='pdbligand=NAT:'>NAT</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Q0B OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Buser, C | + | [[Category: Buser, C A.]] |
[[Category: Halczenko, W.]] | [[Category: Halczenko, W.]] | ||
| - | [[Category: Hartman, G | + | [[Category: Hartman, G D.]] |
[[Category: Homnick, C.]] | [[Category: Homnick, C.]] | ||
| - | [[Category: Huber, H | + | [[Category: Huber, H E.]] |
| - | [[Category: Kuo, L | + | [[Category: Kuo, L C.]] |
[[Category: Sardana, V.]] | [[Category: Sardana, V.]] | ||
[[Category: Xu, B.]] | [[Category: Xu, B.]] | ||
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[[Category: motor protein]] | [[Category: motor protein]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:34:29 2008'' |
Revision as of 12:34, 21 February 2008
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Crystal structure of the motor protein KSP in complex with ADP and monastrol
Overview
We report here the first inhibitor-bound structure of a mitotic motor protein. The 1.9 A resolution structure of the motor domain of KSP, bound with the small molecule monastrol and Mg2+ x ADP, reveals that monastrol confers inhibition by "induced-fitting" onto the protein some 12 A away from the catalytic center of the enzyme, resulting in the creation of a previously non-existing binding pocket. The structure provides new insights into the biochemical and mechanical mechanisms of the mitotic motor domain. Inhibition of KSP provides a novel mechanism to arrest mitotic spindle formation, a target of several approved and investigative anti-cancer agents. The structural information gleaned from this novel pocket offers a new angle for the design of anti-mitotic agents.
About this Structure
1Q0B is a Single protein structure of sequence from Homo sapiens with , and as ligands. Full crystallographic information is available from OCA.
Reference
Inhibition of a mitotic motor protein: where, how, and conformational consequences., Yan Y, Sardana V, Xu B, Homnick C, Halczenko W, Buser CA, Schaber M, Hartman GD, Huber HE, Kuo LC, J Mol Biol. 2004 Jan 9;335(2):547-54. PMID:14672662
Page seeded by OCA on Thu Feb 21 14:34:29 2008
Categories: Homo sapiens | Single protein | Buser, C A. | Halczenko, W. | Hartman, G D. | Homnick, C. | Huber, H E. | Kuo, L C. | Sardana, V. | Xu, B. | Yan, Y. | ADP | MG | NAT | Cell cycle | Monastrol | Motor protein
