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

Clusan, Léa ; Le Goff, Pascale ; Flouriot, Gilles ; Pakdel, Farzad

International journal of molecular sciences, 2021-01, Vol.22 (2), p.756 [Periódico revisado por pares]

Switzerland: MDPI AG

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Título:
A Closer Look at Estrogen Receptor Mutations in Breast Cancer and Their Implications for Estrogen and Antiestrogen Responses
Autor: Clusan, Léa ; Le Goff, Pascale ; Flouriot, Gilles ; Pakdel, Farzad
Assuntos: Animals ; Antiestrogens ; Antineoplastic Agents, Hormonal - pharmacology ; Antineoplastic Agents, Hormonal - therapeutic use ; Binding sites ; Biomarkers, Tumor ; Breast cancer ; Breast Neoplasms - drug therapy ; Breast Neoplasms - etiology ; Breast Neoplasms - metabolism ; Breast Neoplasms - pathology ; Carcinogenesis ; Carcinogens ; Cell growth ; Cell proliferation ; Disease Management ; Disease Susceptibility ; endocrine resistance ; Endocrine therapy ; Estrogen Antagonists - pharmacology ; Estrogen Antagonists - therapeutic use ; estrogen receptor ; Estrogen Receptor alpha - antagonists & inhibitors ; Estrogen Receptor alpha - chemistry ; Estrogen Receptor alpha - genetics ; Estrogen Receptor alpha - metabolism ; Estrogen receptors ; Estrogens ; Estrogens - pharmacology ; Estrogens - therapeutic use ; Evolution ; Female ; Gene amplification ; Gene expression ; Growth factors ; Humans ; Kinases ; Life Sciences ; Ligands ; Medical prognosis ; Metastases ; Metastasis ; Molecular Targeted Therapy ; Mutation ; Mutation, Missense ; Proteins ; receptor folding ; Receptors, Estrogen - antagonists & inhibitors ; Receptors, Estrogen - chemistry ; Receptors, Estrogen - genetics ; Receptors, Estrogen - metabolism ; Review ; Silent Mutation ; Structure-Activity Relationship ; Tumors
É parte de: International journal of molecular sciences, 2021-01, Vol.22 (2), p.756
Descrição: 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.
Editor: Switzerland: MDPI AG
Idioma: Inglês

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

Clusan, Léa ; Le Goff, Pascale ; Flouriot, Gilles ; Pakdel, Farzad

Switzerland: MDPI AG

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