组蛋白去乙酰化酶抑制剂在HR阳性HER-2阴性晚期乳腺癌的研究进展

Research progress of histone deacetylase inhibitors in HR positive HER-2 negative advanced breast cancer

摘要: 组蛋白去乙酰化酶（histone deacetylase，HDAC）是可调节表观遗传学改变的组蛋白修饰酶，在一些肿瘤中HDACs被异常激活，与肿瘤进展和耐药密切相关。HDAC抑制剂（HDAC inhibitor，HDACi）通过调节肿瘤细胞的表观遗传属性，靶向性控制肿瘤细胞增殖、调节肿瘤细胞周期及修复DNA损伤。HDACi可抑制多个乳腺癌致癌信号通路，从而有可能逆转激素受体（hormone receptor，HR）阳性HER-2阴性乳腺癌的治疗耐药。本文将对HDACi在HR阳性HER-2阴性晚期乳腺癌治疗方面进行综述，探讨其在乳腺癌治疗领域中的应用前景。

Abstract: Histone deacetylases (HDACs) are histone modifying enzymes that can modulate epigenetic changes. HDACs are abnormally activated in some tumors, and their elevated expression correlates closely with tumor progression and drug resistance. HDAC inhibitors (HDACi) regulate epigenetic modifications in tumor cells controlling tumor cell proliferation, cell cycle, and DNA damage repair. HDACi can inhibit multiple oncogenic signaling pathways in breast cancer, which may reverse treatment resistance in hormone receptor (HR) positive human epidermal growth factor receptor-2 (HER-2) negative breast cancer. This review summarizes research progress regarding using HDACi to treat HR positive HER-2 negative advanced breast cancer and discusses the prospects of its application in breast cancer treatment.