Androgen Receptor Ligands: Agonists and Antagonists

The document from 2018 examines the role of the androgen receptor (AR) in the body, which is activated by hormones such as testosterone and dihydrotestosterone (DHT). These hormones lead to changes in the AR that affect gene regulation. AR agonists, including natural hormones and synthetic compounds like mesterolone and selective androgen receptor modulators (SARMs), play a key role in male development, reproductive health, and other bodily functions. The document also discusses the concept of intracrinology, particularly in the prostate and its relevance to prostate cancer. It compares the binding affinities of various synthetic AR agonists to DHT. Additionally, AR antagonists are highlighted for their therapeutic potential in treating conditions like prostate cancer, acne, and androgenic alopecia, noting the difference between steroidal and non-steroidal inhibitors.