| Literature DB >> 16213716 |
Paul A Brough1, Xavier Barril, Mandy Beswick, Brian W Dymock, Martin J Drysdale, Lisa Wright, Kate Grant, Andrew Massey, Allan Surgenor, Paul Workman.
Abstract
Information from X-ray crystal structures of Hsp90 inhibitors bound to the human Hsp90 molecular chaperone was used to assist in the design of 3-(5-chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as novel inhibitors of Hsp90. Accessing an extra interaction with the protein via Phe138 gave a significant increase in binding potency compared to similar analogues that do not make this interaction.Entities:
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Year: 2005 PMID： 16213716 DOI： 10.1016/j.bmcl.2005.08.091
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823