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
Letters in Drug Design & Discovery
Title: 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
Volume: 6 Issue: 7
Author(s): Kruti Shah, Moniola S. Olusanjo, Tim Cartledge, Caroline P. Owen and Sabbir Ahmed
Affiliation:
Keywords: 17β-hydroxysteroid dehydrogenase, Type 3, Androgen ablation, Enzyme inhibition, Methanesulfonate
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.
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Shah Kruti, Olusanjo S. Moniola, Cartledge Tim, Owen P. Caroline and Ahmed Sabbir, 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, Letters in Drug Design & Discovery 2009; 6 (7) . https://dx.doi.org/10.2174/157018009789108259
DOI https://dx.doi.org/10.2174/157018009789108259 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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