Selective degradation of the estrogen receptor in the treatment of cancers

Estrogen receptor subtype ? (ER?) plays key roles in breast cancers, and has been a target for endocrine therapy for a long time. Unfortunately, long-term treatment by Aromatase Inhibitors (AIs) or Selective Estrogen Receptor Modulators (SERMs) could cause drug resistance and also would increase the risk for uterine cancer. Therefore, novel anti-breast cancer drugs based on different mechanisms of action have received significant attention, especially through the strategies of selective degradation of ER. In this article, the latest research progress of selective targeting ER for degradation, including Selective ER Downregulators (SERDs), Proteolysis Targeting Chimaeras (PROTACs) and other techniques, was reviewed, and the applications and problems to be solved were prospected.

Automated summary

ERα plays a key role in breast cancer and has been a target for endocrine therapy, but long-term treatment with AIs or SERMs may lead to drug resistance and increase the risk of uterine cancer. Therefore, novel anti-breast cancer drugs based on different mechanisms of action, especially through selective degradation of ER, have attracted significant attention.