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:School of Science, University of the West of Scotland, High Street, Paisley, PA1 2BE, Scotland, UK.
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.