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<p>Estrogen receptor α (ERα) is a key therapeutic target in ER-positive breast cancer. Structurally, ERα contains activation function (AF) domains that drives breast cancer proliferation, metastasis, and drug resistance through classical genomic, non-genomic, and ligand-independent signaling pathways. Clinically approved and investigational drugs targeting Erα include selective estrogen receptor modulators (SERMs), selective estrogen receptor downregulators/degraders (SERDs), and novel strategies such as proteolysis-targeting chimeras (PROTACs). Current research focuses on overcoming endocrine resistance via combination therapies targeting mutations in <i>ESR1</i>, the gene encoding ERα, non-genomic signaling pathways, and the tumor microenvironment, which may advance precision medicine in breast cancer. This article summarizes recent advances in ERα-targeting inhibitors and their therapeutic implications, to provide potential precision therapeutic strategies for breast cancer patients with ER positive.</p>

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Targeting estrogen receptor alpha in breast cancer for novel therapies resistance mechanisms and future directions

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年12月31日

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  • Bing-Xuan Wu,
  • Hua-Tao Wu,
  • Yang-Zheng Lan,
  • Wen-Jia Chen,
  • Xin-Ning Yu,
  • Jia-Wei Liu,
  • Jing Liu

摘要

Estrogen receptor α (ERα) is a key therapeutic target in ER-positive breast cancer. Structurally, ERα contains activation function (AF) domains that drives breast cancer proliferation, metastasis, and drug resistance through classical genomic, non-genomic, and ligand-independent signaling pathways. Clinically approved and investigational drugs targeting Erα include selective estrogen receptor modulators (SERMs), selective estrogen receptor downregulators/degraders (SERDs), and novel strategies such as proteolysis-targeting chimeras (PROTACs). Current research focuses on overcoming endocrine resistance via combination therapies targeting mutations in ESR1, the gene encoding ERα, non-genomic signaling pathways, and the tumor microenvironment, which may advance precision medicine in breast cancer. This article summarizes recent advances in ERα-targeting inhibitors and their therapeutic implications, to provide potential precision therapeutic strategies for breast cancer patients with ER positive.