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Penicillin inhibitors of purple acid phosphatase.
MedLine Citation:
PMID:  22366658     Owner:  NLM     Status:  Publisher    
Purple acid phosphatases (PAPs) are binuclear metallohydrolases that have a multitude of biological functions and are found in fungi, bacteria, plants and animals. In mammals, PAP activity is linked with bone resorption and over-expression can lead to bone disorders such as osteoporosis. PAP is therefore an attractive target for the development of drugs to treat this disease. A series of penicillin conjugates, in which 6-aminopenicillanic acid was acylated with aromatic acid chlorides, has been prepared and assayed against pig PAP. The binding mode of most of these conjugates is purely competitive, and some members of this class have potencies comparable to the best PAP inhibitors yet reported. The structurally related penicillin G was shown to be neither an inhibitor nor a substrate for pig PAP. Molecular modelling has been used to examine the binding modes of these compounds in the active site of the enzyme and to rationalise their activities.
Faridoon; Waleed M Hussein; Nazar Ul Islam; Luke W Guddat; Gerhard Schenk; Ross P McGeary
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-2-4
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  -     Publication Date:  2012 Feb 
Date Detail:
Created Date:  2012-2-27     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Crown Copyright © 2012. Published by Elsevier Ltd. All rights reserved.
The University of Queensland, School of Chemistry and Molecular Biosciences, Brisbane, Qld 4072, Australia; Institute of Chemical Sciences, University of Peshawar, Peshawar-25120, Pakistan.
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