1q0b: Difference between revisions
No edit summary |
No edit summary |
||
| Line 1: | Line 1: | ||
[[Image:1q0b.gif|left|200px]] | [[Image:1q0b.gif|left|200px]] | ||
'''Crystal structure of the motor protein KSP in complex with ADP and monastrol''' | {{Structure | ||
|PDB= 1q0b |SIZE=350|CAPTION= <scene name='initialview01'>1q0b</scene>, resolution 1.9Å | |||
|SITE= | |||
|LIGAND= <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ADP:ADENOSINE-5'-DIPHOSPHATE'>ADP</scene> and <scene name='pdbligand=NAT:ETHYL 4-(3-HYDROXYPHENYL)-6-METHYL-2-THIOXO-1,2,3,4-TETRAHYDROPYRIMIDINE-5-CARBOXYLATE'>NAT</scene> | |||
|ACTIVITY= | |||
|GENE= KIF11 OR KNSL1 OR EG5 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |||
}} | |||
'''Crystal structure of the motor protein KSP in complex with ADP and monastrol''' | |||
==Overview== | ==Overview== | ||
| Line 7: | Line 16: | ||
==About this Structure== | ==About this Structure== | ||
1Q0B is a [ | 1Q0B is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Q0B OCA]. | ||
==Reference== | ==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:[http:// | 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:[http://www.ncbi.nlm.nih.gov/pubmed/14672662 14672662] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| Line 29: | Line 38: | ||
[[Category: motor protein]] | [[Category: motor protein]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 13:31:19 2008'' | ||
Revision as of 11:31, 20 March 2008
| |||||||||||||
| 1q0b, resolution 1.9Å | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Ligands: | MG, ADP and NAT | ||||||||||||
| Gene: | KIF11 OR KNSL1 OR EG5 (Homo sapiens) | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
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. 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 Mar 20 13:31:19 2008
