MTH1是一种DNA氧化损伤修复酶,主要负责“清理”核苷酸池中氧化损伤的脱氧核苷三磷酸(d NTPs),以防其掺入DNA复制中而造成碱基错配。研究表明,MTH1与肿瘤细胞的生存密切相关,而正常细胞的生长与存活则不依赖于MTH1。所以,以MTH1为靶点开展抗肿瘤新药研发,已逐渐受到人们的关注。抑制MTH1,为肿瘤治疗开辟了一条新途经。简介MTH1的结构和功能及其与肿瘤的关联,着重对近年来MTH1抑制剂的发现过程和研究进展作一综述,探究小分子MTH1抑制剂与MTH1蛋白的作用模式,为MTH1抑制剂的设计提供思路。 MTH1 is a DNA oxidative damage repair enzyme that is primarily responsible for the oxidative damage of dNTPs in “clean-up ” nucleotide pools to prevent base-mismatched incorporation into DNA replication. Studies have shown that MTH1 and tumor cell survival are closely related to the normal cell growth and survival is not dependent on MTH1. Therefore, the development of antitumor drug targeting MTH1 has gradually attracted people’s attention. Inhibit MTH1, opened up a new way for cancer treatment. Brief introduction The structure and function of MTH1 and its relation with tumor, focusing on the discovery process and research progress of MTH1 inhibitors in recent years, to explore the mode of action of small molecule MTH1 inhibitor and MTH1 protein for MTH1 inhibitor design Ideas.