2fky

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[[Image:2fky.gif|left|200px]]
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{{Seed}}
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[[Image:2fky.png|left|200px]]
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{{STRUCTURE_2fky| PDB=2fky | SCENE= }}
{{STRUCTURE_2fky| PDB=2fky | SCENE= }}
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'''crystal structure of KSP in complex with inhibitor 13'''
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===crystal structure of KSP in complex with inhibitor 13===
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==Overview==
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The evolution of 2,4-diaryl-2,5-dihydropyrroles as inhibitors of KSP is described. Introduction of basic amide and urea moieties to the dihydropyrrole nucleus enhanced potency and aqueous solubility, simultaneously, and provided compounds that caused mitotic arrest of A2780 human ovarian carcinoma cells with EC(50)s&lt;10nM. Ancillary hERG activity was evaluated for this series of inhibitors.
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The line below this paragraph, {{ABSTRACT_PUBMED_16439123}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16439123 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16439123}}
==About this Structure==
==About this Structure==
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[[Category: Ksp]]
[[Category: Ksp]]
[[Category: Ksp-inhibitor complex]]
[[Category: Ksp-inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:00:45 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 06:22:43 2008''

Revision as of 03:22, 28 July 2008

Image:2fky.png

Template:STRUCTURE 2fky

crystal structure of KSP in complex with inhibitor 13

Template:ABSTRACT PUBMED 16439123

About this Structure

2FKY is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP., Fraley ME, Garbaccio RM, Arrington KL, Hoffman WF, Tasber ES, Coleman PJ, Buser CA, Walsh ES, Hamilton K, Fernandes C, Schaber MD, Lobell RB, Tao W, South VJ, Yan Y, Kuo LC, Prueksaritanont T, Shu C, Torrent M, Heimbrook DC, Kohl NE, Huber HE, Hartman GD, Bioorg Med Chem Lett. 2006 Apr 1;16(7):1775-9. Epub 2006 Jan 24. PMID:16439123

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