2bz5

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{{STRUCTURE_2bz5| PDB=2bz5 | SCENE= }}
{{STRUCTURE_2bz5| PDB=2bz5 | SCENE= }}
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'''STRUCTURE-BASED DISCOVERY OF A NEW CLASS OF HSP90 INHIBITORS'''
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===STRUCTURE-BASED DISCOVERY OF A NEW CLASS OF HSP90 INHIBITORS===
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==Overview==
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Docking-based virtual screening identified 1-(2-phenol)-2-naphthol compounds as a new class of Hsp90 inhibitors of low to sub-micromolar potency. Here we report the binding affinities and cellular activities of several members of this class. A high resolution crystal structure of the most potent compound reveals its binding mode in the ATP binding site of Hsp90, providing a rationale for the observed activity of the series and suggesting strategies for developing compounds with improved properties.
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(as it appears on PubMed at http://www.pubmed.gov), where 16202589 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16202589}}
==About this Structure==
==About this Structure==
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[[Category: Nucleotide-binding]]
[[Category: Nucleotide-binding]]
[[Category: Phosphorylation]]
[[Category: Phosphorylation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 21:00:06 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:14:57 2008''

Revision as of 12:14, 28 July 2008

Template:STRUCTURE 2bz5

STRUCTURE-BASED DISCOVERY OF A NEW CLASS OF HSP90 INHIBITORS

Template:ABSTRACT PUBMED 16202589

About this Structure

2BZ5 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure-based discovery of a new class of Hsp90 inhibitors., Barril X, Brough P, Drysdale M, Hubbard RE, Massey A, Surgenor A, Wright L, Bioorg Med Chem Lett. 2005 Dec 1;15(23):5187-91. Epub 2005 Oct 3. PMID:16202589

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