2bt0

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{{STRUCTURE_2bt0| PDB=2bt0 | SCENE= }}
{{STRUCTURE_2bt0| PDB=2bt0 | SCENE= }}
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'''NOVEL, POTENT SMALL MOLECULE INHIBITORS OF THE MOLECULAR CHAPERONE HSP90 DISCOVERED THROUGH STRUCTURE-BASED DESIGN'''
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===NOVEL, POTENT SMALL MOLECULE INHIBITORS OF THE MOLECULAR CHAPERONE HSP90 DISCOVERED THROUGH STRUCTURE-BASED DESIGN===
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==Overview==
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The crystal structure of a previously reported screening hit 1 (CCT018159) bound to the N terminal domain of molecular chaperone Hsp90 has been used to design 5-amide analogues. These exhibit enhanced potency against the target in binding and functional assays with accompanying appropriate cellular pharmacodynamic changes. Compound 11 (VER-49009) compares favorably with the clinically evaluated 17-AAG.
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(as it appears on PubMed at http://www.pubmed.gov), where 15974572 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15974572}}
==About this Structure==
==About this Structure==
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[[Category: Heat shock]]
[[Category: Heat shock]]
[[Category: Phosphorylation]]
[[Category: Phosphorylation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:45:29 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 10:49:01 2008''

Revision as of 07:49, 28 July 2008

Image:2bt0.png

Template:STRUCTURE 2bt0

NOVEL, POTENT SMALL MOLECULE INHIBITORS OF THE MOLECULAR CHAPERONE HSP90 DISCOVERED THROUGH STRUCTURE-BASED DESIGN

Template:ABSTRACT PUBMED 15974572

About this Structure

2BT0 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design., Dymock BW, Barril X, Brough PA, Cansfield JE, Massey A, McDonald E, Hubbard RE, Surgenor A, Roughley SD, Webb P, Workman P, Wright L, Drysdale MJ, J Med Chem. 2005 Jun 30;48(13):4212-5. PMID:15974572

Page seeded by OCA on Mon Jul 28 10:49:01 2008

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