赖氨酸特异性去甲基化酶 1 有望成为癌症耐药性的新靶点：治疗意义。
Lysine-Specific Demethylase 1 Promises to Be a Novel Target in Cancer Drug Resistance: Therapeutic Implications.
机构信息
State Key Laboratory of Esophageal Cancer Prevention and Treatment, Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, School of Pharmaceutical Science and Institute of Pharmaceutical Science, Zhengzhou University, Zhengzhou, Henan 450001, China.
Key Laboratory of Cardio-Cerebrovascular Drug, China Meheco Topfond Pharmaceutical Company, Zhumadian 463000, China.
出版信息
J Med Chem. 2023 Apr 13;66(7):4275-4293. doi: 10.1021/acs.jmedchem.2c01527. Epub 2023 Apr 4.
Chemotherapy, targeted therapy, and immunotherapy are effective against most tumors, but drug resistance remains a barrier to successful treatment. Lysine-specific demethylase 1 (LSD1), a member of histone demethylation modifications, can regulate invasion, metastasis, apoptosis, and immune escape of tumor cells, which are associated with tumorigenesis and tumor progression. Recent studies suggest that LSD1 ablation regulates resensitivity of tumor cells to anticarcinogens containing immune checkpoint inhibitors (ICIs) via multiple upstream and downstream pathways. In this review, we describe the recent findings about LSD1 biology and its role in the development and progression of cancer drug resistance. Further, we summarize LSD1 inhibitors that have a reversal or resensitive effect on drug resistance and discuss the possibility of targeting LSD1 in combination with other agents to surmount resistance.
化疗、靶向治疗和免疫治疗对大多数肿瘤有效，但药物耐药性仍是成功治疗的障碍。赖氨酸特异性去甲基化酶 1（LSD1）是组蛋白去甲基化修饰的成员，可调节肿瘤细胞的侵袭、转移、凋亡和免疫逃逸，与肿瘤发生和肿瘤进展有关。最近的研究表明，LSD1 缺失通过多种上下游途径调节肿瘤细胞对含有免疫检查点抑制剂（ICI）的抗癌药物的敏感性。在这篇综述中，我们描述了 LSD1 生物学及其在癌症耐药性发展和进展中的作用的最新发现。此外，我们总结了对耐药性具有逆转或敏感作用的 LSD1 抑制剂，并讨论了与其他药物联合靶向 LSD1 以克服耐药性的可能性。
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