Document Detail


Highly selective azadipeptide nitrile inhibitors for cathepsin K: design, synthesis and activity assays.
MedLine Citation:
PMID:  23299878     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
We have developed a series of azadipeptide nitriles with different P3 groups. A triaryl meta-phenyl derivative, compound , was not only a potent inhibitor for cathepsin K (K(i) = 0.0031 nM), but also highly selective over both cathepsins B and S (∼1000-fold). A protein-ligand docking study performed on the series provided a possible explanation why compound could be significantly more potent than the others, especially compound in the same series.
Authors:
Xing-Feng Ren; Hong-Wei Li; Xuexun Fang; Yuqing Wu; Lincong Wang; Shuxue Zou
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-9
Journal Detail:
Title:  Organic & biomolecular chemistry     Volume:  -     ISSN:  1477-0539     ISO Abbreviation:  Org. Biomol. Chem.     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-9     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101154995     Medline TA:  Org Biomol Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
State Key Laboratory of Supramolecular Structure and Materials, Jilin University, No. 2699, Qianjin Street, Changchun 130012, China. yqwu@jlu.edu.cn.
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