Selective Androgen Receptor Modulators

Selective Androgen Receptor Modulators (SARMs) are a class of androgen receptor ligands that bind androgen receptor and display tissue-selective activation of androgenic signaling (1, 2). The initial efforts to develop steroidal SARMs, based on modifications of the testosterone molecule, date back to the 1940s. The modern era of nonsteroidal SARMs was unleashed by independent work at Ligand Pharmaceuticals (3–6) and the University of Tennessee (7, 8). The scientists at Ligand Pharmaceuticals were the first to develop a series of cyclic quinolinones that had anabolic activity on the skeletal muscle and some degree of tissue selectivity (3, 4, 9–13). The discovery by Dalton and Miller that aryl propionamides with structural similarities to bicalutamide and hydroxyflutamide could activate AR-dependent transcriptional activity provided the early lead for the development of diaryl propionamide class of SARMs (7, 8). The decade since these early efforts has witnessed the emergence of a large number of nonsteroidal SARMs from virtually all the major pharmaceutical companies (2). The review will focus on the rationale for SARM development, the molecular basis of androgen action, the mechanistic basis of tissue selectivity, and potential clinical applications for SARMs. (Source: US National Library of Medicine National Institutes of Health - http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2907129/?tool=pubmed) Other sources: http://www.sarmsinfo.com/ http://en.wikipedia.org/wiki/Selective_androgen_receptor_modulator http://www.ncbi.nlm.nih.gov/pubmed/18708695 - test method description