Document Detail


Fragment-based identification of Hsp90 inhibitors.
MedLine Citation:
PMID:  19301319     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Heat shock protein 90 (Hsp90) plays a key role in stress response and protection of the cell against the effects of mutation. Herein we report the identification of an Hsp90 inhibitor identified by fragment screening using a high-concentration biochemical assay, as well as its optimisation by in silico searching coupled with a structure-based drug design (SBDD) approach.
Authors:
John J Barker; Oliver Barker; Roberto Boggio; Viddhata Chauhan; Robert K Y Cheng; Vincent Corden; Stephen M Courtney; Neil Edwards; Virginie M Falque; Fulvia Fusar; Mihaly Gardiner; Estelle M N Hamelin; Thomas Hesterkamp; Osamu Ichihara; Richard S Jones; Owen Mather; Ciro Mercurio; Saverio Minucci; Christian A G N Montalbetti; Annett Müller; Deepti Patel; Banu G Phillips; Mario Varasi; Mark Whittaker; Dirk Winkler; Christopher J Yarnold
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  ChemMedChem     Volume:  4     ISSN:  1860-7187     ISO Abbreviation:  -     Publication Date:  2009 Jun 
Date Detail:
Created Date:  2009-06-03     Completed Date:  2009-08-06     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101259013     Medline TA:  ChemMedChem     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  963-6     Citation Subset:  IM    
Affiliation:
Evotec, 114 Milton Park, Abingdon, Oxfordshire, OX10 4SA UK.
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MeSH Terms
Descriptor/Qualifier:
Binding Sites
Cell Line, Tumor
Computer Simulation
Crystallography, X-Ray
Drug Design
HSP90 Heat-Shock Proteins / antagonists & inhibitors*,  metabolism
Humans
Oximes / chemical synthesis,  chemistry*,  pharmacology
Pyrimidines / chemical synthesis,  chemistry*,  pharmacology
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/HSP90 Heat-Shock Proteins; 0/Oximes; 0/Pyrimidines

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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