雌激素受体在癌症中的作用:特别强调雌激素受体β的治疗潜力

Q4 Pharmacology, Toxicology and Pharmaceutics

Pharmaceutical Sciences Asia Pub Date : 2022-01-01 DOI:10.29090/psa.2022.05.22.042

Emdormi Rymbai, D. Sugumar, Dhritiman Roy, Divakar Selvaraj

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引用次数: 0

摘要

雌激素受体是核受体，在生理和病理上都起着重要作用。雌激素受体亚型目前分为三组:雌激素受体α (ERα)，雌激素受体β (ERβ)和G蛋白偶联雌激素受体1 (GPER1或以前称为GPR30或GPRx，一种膜结合受体)。众所周知，ERα和GPER1的过表达与癌症有关，其中ERα起着最重要的作用。另一方面，人们普遍认为ERβ抑制ERα活性并具有抗癌特性。因此，雌激素受体ERα和ERβ是研究最多的，其中ERα被认为是治疗乳腺癌的治疗靶点。与必须阻断的ERα不同，ERβ在激活时具有抗癌特性。ERβ潜在的抗癌功效已经在一些临床前和临床研究中得到证实。在这篇综述中，我们总结了ERβ和ERβ激动剂在各种癌症中的潜在作用。

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Role of estrogen receptors in cancer: a special emphasis on the therapeutic potential of estrogen receptor β

Estrogen receptors are nuclear receptors that play a major role in both physiology and pathology. Estrogen receptor subtypes are currently divided into three groups: estrogen receptor alpha (ERα), estrogen receptor beta (ERβ), and G protein-coupled estrogen receptor 1 (GPER1 or formerly known as GPR30 or GPRx, a membrane-bound receptor). Overexpression of ERα and GPER1 are known to contribute to cancer, with ERα playing the most important impact. On the other hand, it is commonly acknowledged that ERβ inhibits ERα activity and has anti-cancer properties. As a result, the estrogen receptors ERα and ERβ are the most investigated, with ERα being recognized therapeutically as a therapeutic target for breast cancer. Unlike ERα, which must be blocked, ERβ is a target that has anti-cancer properties when activated. The potential anti-cancer efficacy of ERβ has been demonstrated in several pre-clinical and clinical investigations. In this review, we summarize the potential role of ERβ and ERβ agonists in various cancers.

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来源期刊

Pharmaceutical Sciences Asia Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

0.90

自引率

0.00%

发文量

期刊介绍： The Pharmaceutical Sciences Asia (PSA) journal is a double-blinded peer-reviewed journal in English published quarterly, by the Faculty of Pharmacy, Mahidol University, Thailand. The PSA journal is formerly known as Mahidol University Journal of Pharmaceutical Sciences and committed to the timely publication of innovative articles and reviews. This journal is available in both printed and electronic formats. The PSA journal aims at establishing a publishing house that is open to all. It aims to disseminate knowledge; provide a learned reference in the field; and establish channels of communication between academic and research expert, policy makers and executives in industry and investment institutions. The journal publishes research articles, review articles, and scientific commentaries on all aspects of the pharmaceutical sciences and multidisciplinary field in health professions and medicine. More specifically, the journal publishes research on all areas of pharmaceutical sciences and related disciplines: Clinical Pharmacy Drug Synthesis and Discovery Targeted-Drug Delivery Pharmaceutics Biopharmaceutical Sciences Phytopharmaceutical Sciences Pharmacology and Toxicology Pharmaceutical Chemistry Nutraceuticals and Functional Foods Natural Products Social, Economic, and Administrative Pharmacy Clinical Drug Evaluation and Drug Policy Making Antimicrobials, Resistance and Infection Control Pharmacokinetics and Pharmacodynamics.