Estrogen receptor α revised: Expression, structure, function, and stability

Makoto Habara

doi:10.1002/bies.202200148

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Estrogen receptor α revised: Expression, structure, function, and stability

2022-10-03

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Makoto Habara

Midori Shimada *

DOI：10.1002/bies.202200148

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Abstract

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Estrogen receptor alpha (ER alpha) is a ligand-dependent transcription factor that regulates the expression of estrogen-responsive genes. Approximately 70% of patients with breast cancer are ER alpha positive. Estrogen stimulates cancer cell proliferation and contributes to tumor progression. Endocrine therapies, which suppress the ER alpha 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 ER alpha is essential to overcome the resistance to treatment. This review focuses on the regulation of ER alpha expression, including copy number variation, epigenetic regulation, transcriptional regulation, and stability, as well as functions from the point of view post-translational modifications.

Keywords:

breast cancer

calcineurin

estrogen receptor alpha

FKBP

phosphorylation

post-translational modification

ubiquitination