Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
Benxi Institute of Pharmaceutical Research, Shenyang Pharmaceutical University, Benxi, People's Republic of China.
J Exp Clin Cancer Res. 2020 Aug 28;39(1):173. doi: 10.1186/s13046-020-01682-z.
A number of novel anticancer drugs have been developed in recent years. However, the mortality of cancer patients remains high because of the emergence of drug resistance. It was reported that drug resistance might involved in changes in gene expression without changing genotypes, which is similar to epigenetic modification. Some studies indicated that targeting histone methyltransferase can reverse drug resistance. Hence, the use of histone methyltransferase inhibitors or histone demethylase inhibitors opens new therapeutic approaches for cancer treatment. While the relationship between histone methyltransferase and tumor resistance has been determined, there is a lack of updated review on the association between them. In this review, we summarized the mechanisms of histone methyltransferases in cancer drug resistance and the therapeutic strategies of targeting histone methyltransferase to reverse drug resistance.
近年来已经开发出许多新型抗癌药物。然而，由于耐药性的出现，癌症患者的死亡率仍然很高。有报道称，耐药性可能涉及基因表达的变化而基因型不变，这类似于表观遗传修饰。一些研究表明，靶向组蛋白甲基转移酶可以逆转耐药性。因此，使用组蛋白甲基转移酶抑制剂或组蛋白去甲基化酶抑制剂为癌症治疗开辟了新的治疗方法。虽然已经确定了组蛋白甲基转移酶与肿瘤耐药性之间的关系，但缺乏关于它们之间关联的最新综述。在这篇综述中，我们总结了组蛋白甲基转移酶在癌症药物耐药性中的作用机制以及靶向组蛋白甲基转移酶逆转耐药性的治疗策略。
