The Korean Journal of Sports Medicine

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Fig. 2.

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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 https://doi.org/10.5763/kjsm.2022.40.2.67
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