These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.
Pubmed for Handhelds
PUBMED FOR HANDHELDS
Search MEDLINE/PubMed
Title: Structure-based discovery of a new class of Hsp90 inhibitors. Author: Barril X, Brough P, Drysdale M, Hubbard RE, Massey A, Surgenor A, Wright L. Journal: Bioorg Med Chem Lett; 2005 Dec 01; 15(23):5187-91. PubMed ID: 16202589. Abstract: 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.[Abstract] [Full Text] [Related] [New Search]