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Nucl Recept Signal. 2008;6:e010. doi: 10.1621/nrs.06010. Epub 2008 Nov 26.

Selective androgen receptor modulators in preclinical and clinical development.

Author information

1
Preclinical Research and Development, GTx, Inc., Memphis, Tennessee, USA.

Abstract

Androgen receptor (AR) plays a critical role in the function of several organs including primary and accessory sexual organs, skeletal muscle, and bone, making it a desirable therapeutic target. Selective androgen receptor modulators (SARMs) bind to the AR and demonstrate osteo- and myo-anabolic activity; however, unlike testosterone and other anabolic steroids, these nonsteroidal agents produce less of a growth effect on prostate and other secondary sexual organs. SARMs provide therapeutic opportunities in a variety of diseases, including muscle wasting associated with burns, cancer, or end-stage renal disease, osteoporosis, frailty, and hypogonadism. This review summarizes the current standing of research and development of SARMs, crystallography of AR with SARMs, plausible mechanisms for their action and the potential therapeutic indications for this emerging class of drugs.

PMID:
19079612
PMCID:
PMC2602589
DOI:
10.1621/nrs.06010
[Indexed for MEDLINE]
Free PMC Article

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