Aldo-keto reductase 1C3—Assessment as a new target for the treatment of endometriosis

Tea Lanišnik Rižner, T.M. Penning, Trevor M Penning
Pharmacological research · 2019 · vol. 152 , pp. 104446 · doi:10.1016/j.phrs.2019.104446 · PMID:31546014 · W2973660184
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This review assesses the aldo-keto reductase 1C3 enzyme as a potential therapeutic target for endometriosis, examining its role in pathophysiology and the efficacy of its inhibitors.

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Abstract

Endometriosis is a common gynecological disorder, which is treated surgically and/ or pharmacologically with an unmet clinical need for new therapeutics. A completed phase I trial and a recent phase II trial that investigated the steroidal aldo-keto reductase 1C3 (AKR1C3) inhibitor BAY1128688 in endometriosis patients prompted this critical assessment on the role of AKR1C3 in endometriosis. This review includes an introduction to endometriosis with emphasis on the roles of prostaglandins and progesterone in its pathophysiology. This is followed by an overview of the major enzymatic activities and physiological functions of AKR1C3 and of the data published to date on the expression of AKR1C3 in endometriosis at the mRNA and protein levels. The review concludes with the rationale for using AKR1C3 inhibitors, a discussion of the effects of AKR1C3 inhibition on the pathophysiology of endometriosis and a brief overview of other drugs under clinical investigation for this indication.

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Condition tags

endometriosis

MeSH descriptors

Aldo-Keto Reductase Family 1 Member C3 Endometriosis Aldo-Keto Reductase Family 1 Member C3 Aldo-Keto Reductase Family 1 Member C3 Animals Endometriosis Endometriosis Endometrium Endometrium Female Humans

Citation neighborhood

Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. [ expand to 2 hops ] — adds papers reached through this work's immediate citers/citees. Heavier; up to 60 extra dots.

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Cited by (10)

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