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A Closer Look at Estrogen Receptor Mutations in Breast Cancer and Their Implications for Estrogen and Antiestrogen Responses

Inserm, EHESP, Irset (Institut de Recherche en Santé, Environnement et Travail)-UMR_S1085, Rennes University, F-35000 Rennes, France
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Int. J. Mol. Sci. 2021, 22(2), 756; https://doi.org/10.3390/ijms22020756
Received: 26 November 2020 / Revised: 29 December 2020 / Accepted: 31 December 2020 / Published: 13 January 2021
(This article belongs to the Special Issue The Role of Estrogen Receptors in Health and Disease)
Breast cancer (BC) is the most common cancer among women worldwide. More than 70% of BC cases express estrogen receptor alpha (ERα), a central transcription factor that stimulates the proliferation of breast cancer cells, usually in the presence of estrogen. While most cases of ER-positive BC initially respond to antiestrogen therapies, a high percentage of cases develop resistance to treatment over time. The recent discovery of mutated forms of ERα that result in constitutively active forms of the receptor in the metastatic-resistance stage of BC has provided a strong rationale for the development of new antiestrogens. These molecules targeting clinically relevant ERα mutants and a combination with other pharmacological inhibitors of specific pathways may constitute alternative treatments to improve clinical practice in the fight against metastatic-resistant ER-positive BC. In this review, we summarize the latest advances regarding the particular involvement of point mutations of ERα in endocrine resistance. We also discuss the involvement of synonymous ERα mutations with respect to co-translational folding of the receptor and ribosome biogenesis in breast carcinogenesis. View Full-Text
Keywords: estrogen receptor; breast cancer; endocrine resistance; mutation; receptor folding estrogen receptor; breast cancer; endocrine resistance; mutation; receptor folding
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MDPI and ACS Style

Clusan, L.; Le Goff, P.; Flouriot, G.; Pakdel, F. A Closer Look at Estrogen Receptor Mutations in Breast Cancer and Their Implications for Estrogen and Antiestrogen Responses. Int. J. Mol. Sci. 2021, 22, 756. https://doi.org/10.3390/ijms22020756

AMA Style

Clusan L, Le Goff P, Flouriot G, Pakdel F. A Closer Look at Estrogen Receptor Mutations in Breast Cancer and Their Implications for Estrogen and Antiestrogen Responses. International Journal of Molecular Sciences. 2021; 22(2):756. https://doi.org/10.3390/ijms22020756

Chicago/Turabian Style

Clusan, Léa; Le Goff, Pascale; Flouriot, Gilles; Pakdel, Farzad. 2021. "A Closer Look at Estrogen Receptor Mutations in Breast Cancer and Their Implications for Estrogen and Antiestrogen Responses" Int. J. Mol. Sci. 22, no. 2: 756. https://doi.org/10.3390/ijms22020756

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