Development of a biological screening system for the evaluation of highly active and selective 17beta-HSD1-inhibitors as potential therapeutic agents

Patricia Kruchten, Ruth Werth, Sandrine Marchais-Oberwinkler, Martin Frotscher, Rolf W Hartmann
Molecular and cellular endocrinology · 2009 · doi:10.1016/j.mce.2008.09.035 · PMID:18984028
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This study developed and applied a biological screening system to identify potent and selective 17beta-HSD1 inhibitors, discovering four promising compounds with good initial pharmacokinetic profiles.

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Abstract

17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyses the intracellular conversion of oestrone (E1) to oestradiol (E2). E2 is known to be involved in the development and progression of breast cancer and endometriosis. Since 17beta-HSD1 is overexpressed in these oestrogen-dependent diseases, inhibition of this enzyme may be a more target-directed therapeutical approach compared to established medical treatments. For the identification of highly active and selective 17beta-HSD1-inhibitors that are suitable for application as potential therapeutics, there is a need for an appropriate, efficient and reliable screening system. Here, we report the development and application of our screening system using our in house library of potential 17beta-HSD1-inhibitors. Four potent and selective compounds with a good first pharmacokinetic profile were identified.
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Condition tags

endometriosis

MeSH descriptors

17-Hydroxysteroid Dehydrogenases Drug Evaluation, Preclinical Enzyme Inhibitors Enzyme Inhibitors 17-Hydroxysteroid Dehydrogenases Animals Cell Line, Tumor Drug Evaluation, Preclinical Enzyme Inhibitors Estradiol Estradiol Estradiol Estrone Estrone Estrone Humans Male Rats Rats, Wistar

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Source provenance

europepmc
last seen: 2026-06-13T06:22:48.782012+00:00
pubmed
last seen: 2026-05-13T22:14:24.299271+00:00
unpaywall
last seen: 2026-05-14T19:30:52.867331+00:00
License: public-domain-us · commercial use OK · attribution required
Courtesy of the U.S. National Library of Medicine