（1. 广东药科大学生命科学与生物制药学院，广州 510006；2. 广州新华学院健康学院，广州 510520）

摘　要：乳腺癌是世界范围内最常见的恶性肿瘤之一，在女性群体中发病率较高。作为IIa组蛋白去乙酰化酶（HDACs），组蛋白去乙酰化酶5（HDAC5）在乳腺癌患者和健康人群中的表达存在巨大的差异，从而成为在乳腺癌乃至其他癌症中具有潜在价值的生物标志物之一，被认为是抗癌药物的可靠分子治疗靶点。本文将对HDAC5的结构表征和其在乳腺癌发生发展中的作用，以及HDAC5抑制剂的应用作一简要总结，并为早期乳腺癌HDACs的检测、HDACs抑制剂（HDACi）的设计以及与HDACi联用的相关药物作用靶点等方面提供可行性建议，以期为乳腺癌肿瘤治疗提供理论策略参考。

关键词：乳腺癌；组蛋白去乙酰化酶；组蛋白去乙酰化酶5；组蛋白去乙酰化酶5抑制剂；药物作用靶点

中图分类号：R73                              文献标志码：ADOI：10.3969/j.issn.1007-7146.2024.02.002

(1. College of Life Science and Biopharmaceutical Science, Guangdong Pharmaceutical University, Guangzhou 510006, China; 2. School of Health sciences, Guangzhou Xinhua University, Guangzhou 510520, China)

Abstract: Breast cancer ranks as one of the most prevalent malignancies globally, predominantly affecting the female population. Notably, the expression of class IIa histone deacetylases (HDACs), particularly histone deacetylase 5 (HDAC5), exhibits significant variation between breast cancer patients and healthy individuals. This differential expression positions HDAC5 as a promising biomarker for breast cancer and potentially other cancer types. Furthermore, HDAC5 has emerged as a credible molecular target for anticancer therapeutics. This review aims to concisely summarize the structural characteristics of HDAC5, its contributory role in the pathogenesis of breast cancer, and the therapeutic potential of HDAC5 inhibitors. We will discuss the feasibility of detecting HDACs, designing histonedeacetylase inhibitors (HDACi), and identifying effective drug targets in conjunction with HDACi. Our goal is to offer strategic insights for advancing breast cancer treatment, focusing on the application of HDACi in managing breast cancer tumors.

Key words: breast cancer; histone deacetylases; histone deacetylases 5; histone deacetylases 5 inhibitor; drug action targets

（Acta Laser Biology Sinica, 2024, 33(2): 108-114）