1yrs: Difference between revisions
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==Overview== | ==Overview== | ||
Optimization of high-throughput screening (HTS) hits resulted in the | 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. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Breslin, M | [[Category: Breslin, M J.]] | ||
[[Category: Buser, C | [[Category: Buser, C A.]] | ||
[[Category: Coleman, P | [[Category: Coleman, P J.]] | ||
[[Category: Cox, C | [[Category: Cox, C D.]] | ||
[[Category: Hamilton, K.]] | [[Category: Hamilton, K.]] | ||
[[Category: Hartman, G | [[Category: Hartman, G D.]] | ||
[[Category: Kohl, N | [[Category: Kohl, N E.]] | ||
[[Category: Kuo, L | [[Category: Kuo, L C.]] | ||
[[Category: Mariano, B | [[Category: Mariano, B J.]] | ||
[[Category: Torrent, M.]] | [[Category: Torrent, M.]] | ||
[[Category: Walsh, E | [[Category: Walsh, E S.]] | ||
[[Category: Yan, Y.]] | [[Category: Yan, Y.]] | ||
[[Category: ADP]] | [[Category: ADP]] | ||
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[[Category: cell cycle]] | [[Category: cell cycle]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:08:31 2008'' | ||
