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Abstract
Steroid sulfatase (STS), a microsomal enzyme catalysing the hydrolysis of the sulfate esters of 3-hydroxy steroids, has received considerable attention as an attractive drug target. It is crucial for the local production of active oestrogens and androgens from their systemic circulating sulfated precursor, namely oestrone sulfate (E1S) and dehydroepiandrosterone sulfate (DHEAS), which are involved in the pathogenesis of a number of diseases. STS inhibitors have been proposed for the treatment of breast, endometrial and prostate cancer, and for androgen-dependent skin diseases such as alopecia, hirsutism and acne. In addition to various classes of potent irreversible arylsulfamate-based inhibitors, recently novel chemotypes of reversible inhibitors originating from high-throughput screening (HTS) were discovered. All STS inhibitors to date are in the preclinical stage, with the exception of 667COUMATE, which is presently in a Phase I clinical trial. In this review the latest patent disclosures and literature in the field of STS inhibitors are summarised.