Therapeutic Strategies to Target the Androgen Receptor

July 2022 in “ Journal of Medicinal Chemistry ”

Weiguo Xiang, Shaomeng Wang

androgen receptor AR agonists AR antagonists selective AR degraders SARDs heterobifunctional degrader molecules

TLDR Therapies targeting the androgen receptor are being developed to treat prostate cancer and improve bone and muscle health.

The document reviewed therapeutic strategies targeting the androgen receptor (AR), which is crucial for muscle and bone maintenance, male sexual functions, and prostate cancer progression. AR agonists were used to treat bone loss and muscle atrophy, while AR antagonists were developed for prostate cancer, including metastatic castration-resistant prostate cancer (mCRPC). Selective AR degraders (SARDs) and heterobifunctional degrader molecules were also explored, with four compounds in clinical development for prostate cancer treatment. The review summarized various compounds targeting AR and highlighted current research frontiers in this therapeutic area.

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