Department of Veterinary Biochemistry, Yamaguchi University, Yamaguchi, Yamaguchi, Japan.
Bioessays. 2022 Dec;44(12):e2200148. doi: 10.1002/bies.202200148. Epub 2022 Oct 3.
Estrogen receptor α (ERα) is a ligand-dependent transcription factor that regulates the expression of estrogen-responsive genes. Approximately 70% of patients with breast cancer are ERα positive. Estrogen stimulates cancer cell proliferation and contributes to tumor progression. Endocrine therapies, which suppress the ERα signaling pathway, significantly improve the prognosis of patients with breast cancer. However, the development of de novo or acquired endocrine therapy resistance remains a barrier to breast cancer treatment. Therefore, understanding the regulatory mechanisms of ERα is essential to overcome the resistance to treatment. This review focuses on the regulation of ERα expression, including copy number variation, epigenetic regulation, transcriptional regulation, and stability, as well as functions from the point of view post-translational modifications.
雌激素受体α（ERα）是一种配体依赖性转录因子，可调节雌激素反应基因的表达。约 70%的乳腺癌患者为 ERα 阳性。雌激素刺激癌细胞增殖，并促进肿瘤进展。内分泌治疗抑制 ERα 信号通路，显著改善乳腺癌患者的预后。然而，新发性或获得性内分泌治疗耐药的发展仍是乳腺癌治疗的障碍。因此，了解 ERα 的调控机制对于克服治疗耐药性至关重要。本综述重点关注 ERα 表达的调控，包括拷贝数变异、表观遗传调控、转录调控和稳定性，以及从翻译后修饰的角度来看的功能。
