Document Detail


The rational design of inhibitors of nitric oxide formation by inducible nitric oxide synthase.
MedLine Citation:
PMID:  17336523     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A series of compounds was rationally designed as inhibitors of dimer formation of the inducible isoform of nitric oxide synthase, and subsequent nitric oxide production. The conformation of two fragments obtained from a crystal structure was utilized to design a tether connecting those same two fragments. The resulting compounds were potent dimerization inhibitors that bound to the enzyme in a similar conformation as the fragments.
Authors:
Marc Whitlow; Marc Adler; David Davey; Qinglan Huang; Sunil Koovakkat; John F Parkinson; Eric Pham; Mark Polokoff; Wei Xu; Shendong Yuan; Gary Phillips
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Publication Detail:
Type:  Journal Article     Date:  2007-02-09
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  17     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2007 May 
Date Detail:
Created Date:  2007-04-06     Completed Date:  2007-07-24     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  2505-8     Citation Subset:  IM    
Affiliation:
Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, USA.
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MeSH Terms
Descriptor/Qualifier:
Binding Sites
Cell Line, Tumor
Chemistry, Pharmaceutical / methods
Crystallization
Crystallography, X-Ray
Dimerization
Drug Design
Enzyme Inhibitors / chemical synthesis*,  pharmacology
Humans
Models, Chemical
Molecular Conformation
Nitric Oxide Synthase Type II / antagonists & inhibitors*
Chemical
Reg. No./Substance:
0/Enzyme Inhibitors; EC 1.14.13.39/Nitric Oxide Synthase Type II

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


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