Selective androgen receptor modulators

Abstract

Androgens regulate diverse physiological processes involving both reproductive and non-reproductive functions. Most of the signalling effects of androgens are mediated through the androgen receptor (AR), a member of the nuclear receptor superfamily of transcription factors. Binding of specific ligands to the AR initiates signalling by translocation of the receptor from the cytoplasmic compartment to the nucleus, its association with co-activator proteins and control of target gene expression. In this article, we review recent patent publications on selective androgen receptor modulators (SARMs) with differential effects on non-reproductive target tissues. A number of non-steroidal synthetic compounds, notably tricyclic pyridinodihydroquinoline derivatives, show promising anabolic effects without any significant action on the prostate and seminal vesicles. The selective action of these compounds on muscle and bone tissues implies important clinical applications for these androgen analogues in the treatment of elderly men and patients with wasting diseases. Various potential approaches for the rational design of androgen analogues with SARM function are also discussed.

• androgen
• androgen agonist
• androgen antagonist
• androgen receptor
• selective androgen receptor modulator (SARM)