Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab, 143005, India.
Drug and Pollution Testing Laboratory, Guru Nanak Dev University, Amritsar, Punjab, 143005, India.
Mol Divers. 2021 Feb;25(1):603-624. doi: 10.1007/s11030-020-10133-y. Epub 2020 Sep 4.
Breast cancer is the most prominent, frequently diagnosed and leading cause of death among women. Estrogen is an agonist of estrogen receptor alpha (ER-α), expressed in mammary glands and is responsible for initiating many signalling pathways that lead to differentiation and development of breast tissue. Any mutations in these signalling pathways result in irregular growth of mammary tissue, leading to the development of tumour or cancer. All these observations attract the attention of researchers to antagonize ER-α receptor either by developing selective estrogen receptor modulators or by selective estrogen receptor degraders. Therefore, this article provides a brief overview of various factors that are responsible for provoking breast cancer in women and design strategies recently used by the various research groups across the world for antagonizing or demodulating ER-α.
乳腺癌是女性中最突出、最常被诊断出的死因。雌激素是雌激素受体 alpha（ER-α）的激动剂，在乳腺中表达，负责启动许多信号通路，导致乳腺组织的分化和发育。这些信号通路中的任何突变都会导致乳腺组织的不规则生长，导致肿瘤或癌症的发展。所有这些观察结果都引起了研究人员的注意，他们试图通过开发选择性雌激素受体调节剂或选择性雌激素受体降解剂来拮抗 ER-α 受体。因此，本文简要概述了导致女性乳腺癌的各种因素，并介绍了世界各地不同研究小组最近用于拮抗或调节 ER-α 的设计策略。
