Citrus polymethoxyflavones degrade estrogen receptor-alpha (ERα) and combine with tamoxifen for the treatment of estrogen receptor-positive breast cancer.

ABSTRACT: Estrogen receptor-positive (ER⁺) breast cancer seriously endangers the women's physical and mental health worldwide and ER targeting therapy is vital. Here, we found that a citrus polymethoxyflavones (PMFs)-rich hydrolysate (C-H) and its major components (nobiletin and 3-methoxynobiletin) potently degrade ERα protein via the ubiquitin-proteasome pathway, thereby impairing the proliferation of ER⁺ breast cancer cells. Moreover, our study exhibited that C-H combined with tamoxifen (TAM) inhibited the cell proliferation of ER⁺ breast cancer in vitro. It was further confirmed that C-H decreased tumor growth of ER⁺ breast cancer in tumor-bearing 129 mice in vivo and improved the efficacy of tamoxifen. Our study revealed that the c

SUBMITTER: Wang Y 

PROVIDER: S-EPMC11252954 | biostudies-literature | 2024 Jun

REPOSITORIES: biostudies-literature