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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Biochemical Evaluation of a Series of Methanesulfonate Derivatives of 4-Hydroxyphenyl Ketone as Probes of the Active Site of Type 3 OF 17β-Hydroxysteroid Dehydrogenase Family of Enzymes

Author(s): Kruti Shah, Moniola S. Olusanjo, Tim Cartledge, Caroline P. Owen and Sabbir Ahmed

Volume 6 , Issue 7 , 2009

Page: [518 - 523] Pages: 6

DOI: 10.2174/157018009789108259

Price: $65

Abstract

We report the synthesis, evaluation and rationalisation of the inhibitory activity of a series of compounds as probes of the active site of the type 3 of 17β-hydroxysteroid dehydrogenase (17β-HSD3). Results have provided invaluable insight into the active site (as well as supporting the previously reported model) of 17β-HSD3.

Keywords: 17β-hydroxysteroid dehydrogenase, Type 3, Androgen ablation, Enzyme inhibition, Methanesulfonate


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