Laboratory of Medicinal Chemistry, CHUQ (CHUL)-Research Center (Endocrinology and Genomic Unit) and Laval University (Faculty of Medicine), Québec, Canada.
Steroids. 2011 Sep-Oct;76(10-11):929-48. doi: 10.1016/j.steroids.2011.03.010. Epub 2011 Mar 31.
The steroid sulfatase (STS) plays a major role in the regulation of steroid hormone concentrations in several human tissues and target organs and therefore, represents an interesting target to regulate estrogen and androgen levels implicated in different diseases. In this review article, the emphasis is put on STS inhibitors reported in the fruitful 2000-2010 decade, which consolidated the first ones that were previously developed (1990-1999). The inhibitors reviewed are divided into four categories according to the fact that they are sulfamoylated or not or that they have a steroid nucleus or not. Other topics such as function, localization, structure and mechanism as well as applications of STS inhibitors are also briefly discussed to complement the information on this crucial steroidogenic enzyme and its inhibitors.
甾体硫酸酯酶(STS)在几种人体组织和靶器官中类固醇激素浓度的调节中起着重要作用,因此,它是调节与不同疾病相关的雌激素和雄激素水平的一个有趣的靶点。在这篇综述文章中,重点介绍了在硕果累累的 2000-2010 十年间报道的 STS 抑制剂,这些抑制剂巩固了之前开发的第一批抑制剂(1990-1999 年)。根据它们是否磺酰胺化、是否具有甾体核,将所审查的抑制剂分为四类。还简要讨论了其他主题,如 STS 抑制剂的功能、定位、结构和机制及其应用,以补充有关这种关键的甾体生成酶及其抑制剂的信息。