The Korean Journal of Sports Medicine

Indexed in /covered by CAS, KoreaScience & DOI/Crossref:eISSN 2288-6028   pISSN 1226-3729

Fig. 2.

Download original image
Fig. 2. Potential mechanism of selective androgen receptor modulator (SARM) tissue-selectivity based on the coactivator hypothesis. As shown in box C and D, testosterone exerts approximately equal androgen receptor (AR) agonism in both androgenic tissue (i.e., prostate) and anabolic tissue (i.e., skeletal muscle tissue). This likely results from a similar coregulator recruitment and/or ligand-AR complex conformation in both types of tissues. On the other hand, SARMs appear to have partial agonist/weak antagonist activity on the AR in androgenic tissues as a result of recruiting more corepressors than coactivators compared to testosterone/dihydrotestosterone (DHT) (compare boxes A and C). In anabolic tissues, SARMs are shown to preferentially recruit coactivators over corepressors and exert full AR agonist activity, often with a greater magnitude than anabolic-androgenic steroid in the same tissue (compare boxes B and D). HSP: heat shock proteins, 5AR: 5-α-reductase.
Korean J Sports Med 2022;40:67-85
© 2022 Korean J Sports Med