1yrs: Difference between revisions

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{{STRUCTURE_1yrs|  PDB=1yrs  |  SCENE=  }}  
{{STRUCTURE_1yrs|  PDB=1yrs  |  SCENE=  }}  


'''Crystal structure of KSP in complex with inhibitor 1'''
===Crystal structure of KSP in complex with inhibitor 1===




==Overview==
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Optimization of high-throughput screening (HTS) hits resulted in the discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of KSP. Dihydropyrazole 15 is a potent, cell-active KSP inhibitor that induces apoptosis and generates aberrant mitotic spindles in human ovarian carcinoma cells at low nanomolar concentrations. X-ray crystallographic evidence is presented which demonstrates that these inhibitors bind in an allosteric pocket of KSP distant from the nucleotide and microtubule binding sites.
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{{ABSTRACT_PUBMED_15808464}}


==About this Structure==
==About this Structure==
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[[Category: Yan, Y.]]
[[Category: Yan, Y.]]
[[Category: Cell cycle]]
[[Category: Cell cycle]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 16:41:57 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 12:24:39 2008''

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