Document Detail


Structure based design of 11β-HSD1 inhibitors.
MedLine Citation:
PMID:  20809895     Owner:  NLM     Status:  In-Process    
Abstract/OtherAbstract:
Controlling elevated tissue-specific levels of cortisol may provide a novel therapeutic approach for treating metabolic syndrome. This concept has spurred large scale medicinal chemistry efforts in the pharmaceutical industry for the design of 11β-HSD1 inhibitors. High resolution X-ray crystal structures of inhibitors in complex with the enzyme have facilitated the structure-based design of diverse classes of molecules. A summary of binding modes, trends in structure-activity relationships, and the pharmacodynamic data of inhibitors from each class is presented.
Authors:
Suresh Singh; Colin Tice
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Current pharmaceutical biotechnology     Volume:  11     ISSN:  1873-4316     ISO Abbreviation:  Curr Pharm Biotechnol     Publication Date:  2010 Nov 
Date Detail:
Created Date:  2010-11-16     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  100960530     Medline TA:  Curr Pharm Biotechnol     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  779-91     Citation Subset:  IM    
Affiliation:
Vitae Pharmaceuticals, 502 W. Office Center Drive, Fort Washington, PA 19034, USA. ssingh@vitaerx.com
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