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Steroid sulfatase inhibitors
Author(s) -
Nussbaumer Peter,
Billich Andreas
Publication year - 2004
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.20008
Subject(s) - steroid sulfatase , acne , steroid , enzyme , estrogen , sulfatase , chemistry , androgen , pharmacology , hormone , medicine , biochemistry , dermatology
Steroid sulfatase (STS) regulates the local production of estrogens and androgens from systemic precursors in several tissues. The enzyme catalyzes the hydrolysis of the sulfate esters of 3‐hydroxy steroids, which are inactive transport or precursor forms of the active 3‐hydroxy steroids. STS inhibitors are expected to block the local production and, consequently, to reduce the local levels of the hormones. Therefore, they are considered as potential new therapeutic agents for the treatment of estrogen‐ and androgen‐dependent disorders. Indications range from cancers of the breast, endometrium and prostate to androgenetic alopecia and acne. In this review, we give a comprehensive summary of the current knowledge and problems in the field of medicinal chemistry of STS inhibitors. The various types of inhibitors are presented and their structure‐activity relationships are discussed. In addition to potent arylsulfamate‐based, irreversible inhibitors, novel types of reversible inhibitors were recently discovered. The recent publication of the X‐ray structure of STS will further boost research activities on this attractive target. © 2004 Wiley Periodicals, Inc. Med Res Rev, 24, No. 4, 529–576, 2004