Gao Wenqing, Dalton James T
Division of Pharmaceutics, College of Pharmacy, The Ohio State University, 500 W 12th Avenue, Columbus, OH 43210, USA.
Drug Discov Today. 2007 Mar;12(5-6):241-8. doi: 10.1016/j.drudis.2007.01.003. Epub 2007 Feb 7.
Selective androgen receptor modulators (SARMs) are a novel class of androgen receptor (AR) ligands that might change the future of androgen therapy dramatically. With improved pharmacokinetic characteristics and tissue-selective pharmacological activities, SARMs are expected to greatly extend the clinical applications of androgens to osteoporosis, muscle wasting, male contraception and diseases of the prostate. Mechanistic studies with currently available SARMs will help to define the contributions of differential tissue distribution, tissue-specific expression of 5alpha-reductase, ligand-specific regulation of gene expression and AR interactions with tissue-specific coactivators to their observed tissue selectivity, and lead to even greater expansion of selective anabolic therapies.
选择性雄激素受体调节剂（SARMs）是一类新型雄激素受体（AR）配体，可能会极大地改变雄激素治疗的未来。由于具有改善的药代动力学特性和组织选择性药理活性，预计SARMs将极大地扩展雄激素在骨质疏松症、肌肉萎缩、男性避孕和前列腺疾病方面的临床应用。对现有SARMs进行的机制研究将有助于明确不同组织分布、5α-还原酶的组织特异性表达、基因表达的配体特异性调控以及AR与组织特异性共激活因子的相互作用对其观察到的组织选择性的贡献，并导致选择性合成代谢疗法的进一步扩展。
