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药物研发中的选择性雄激素受体调节剂:药物化学与治疗潜力

Selective androgen receptor modulators in drug discovery: medicinal chemistry and therapeutic potential.

作者信息

Cadilla Rodolfo, Turnbull Philip

机构信息

GlaxoSmithKline Inc, Metabolic and Viral Diseases Drug Discovery, Research Triangle Park, PO Box 13398, NC 27705, USA.

出版信息

Curr Top Med Chem. 2006;6(3):245-70. doi: 10.2174/156802606776173456.

DOI:10.2174/156802606776173456
PMID:16515480
Abstract

Modulation of the androgen receptor has the potential to be an effective treatment for hypogonadism, andropause, and associated conditions such as sarcopenia, osteoporosis, benign prostatic hyperplasia, and sexual dysfunction. Side effects associated with classical anabolic steroid treatments have driven the quest for drugs that demonstrate improved therapeutic profiles. Novel, non-steroidal compounds that show tissue selective activity and improved pharmacokinetic properties have been developed. This review provides an overview of current advances in the development of selective androgen receptor modulators (SARMs).

摘要

雄激素受体的调节有潜力成为治疗性腺功能减退、男性更年期以及诸如肌肉减少症、骨质疏松症、良性前列腺增生和性功能障碍等相关病症的有效方法。与传统合成代谢类固醇治疗相关的副作用推动了对具有改善治疗特性药物的探索。已开发出具有组织选择性活性和改善药代动力学特性的新型非甾体化合物。本综述概述了选择性雄激素受体调节剂(SARMs)开发的当前进展。

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