Rapid Induction of the Unfolded Protein Response and Apoptosis by Estrogen Mimic TTC-352 for the Treatment of Endocrine-Resistant Breast Cancer.

ABSTRACT: Patients with long-term estrogen-deprived breast cancer, after resistance to tamoxifen or aromatase inhibitors develops, can experience tumor regression when treated with estrogens. Estrogen's antitumor effect is attributed to apoptosis via the estrogen receptor (ER). Estrogen treatment can have unpleasant gynecologic and nongynecologic adverse events; thus, the development of safer estrogenic agents remains a clinical priority. Here, we study synthetic selective estrogen mimics (SEM) BMI-135 and TTC-352, and the naturally occurring estrogen estetrol (E₄), which are proposed as safer estrogenic agents compared with 17β-estradiol (E₂), for the treatment of endocrine-resistant breast cancer. TTC-352 and E₄ are being evaluated in breast cancer clinical trials.

SUBMITTER: Abderrahman B 

PROVIDER: S-EPMC7790886 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature