摘要
组蛋白甲基化转移酶(histone methyltransferases,HMTs)是一类抗肿瘤药物作用靶点,目前针对HMTs的小分子抑制剂结构丰富,部分已进入临床试验阶段。HMTs抑制剂不仅在抗肿瘤方面效果显著,同时在抗寄生虫等方面也有活性报道。本文对HMTs进行分类综述,重点关注抑制剂的结构、活性、选择性、临床试验结果以及抗肿瘤以外的新药理活性研究。
Histone methyltransferases(HMTs) are targets of anti-tumor drugs.At present,there are diverse small molecule inhibitors for HMTs,and several of them have been in the stage of clinical trials.It is reported that HMTs inhibitors have shown not only excellent anti-tumor efficacy,but also anti-parasites activity.In this review,classification of HMTs is reviewed.Moreover,small molecule inhibitors of HMTs are summarized,focusing on their structures,activity,selectivity,clinical trial results and non-antitumor activity.
作者
李旺
涂杰
刘娜
盛春泉
LI Wang;TU Jie;LIU Na;SHENG Chun-quan(Department of Medicinal Chemistry,School of Pharmacy,Naval Military Medical University,Shanghai 200433,China)
出处
《中国药物化学杂志》
CAS
CSCD
2021年第2期129-141,共13页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(81725020,81973175)
上海市教委科研创新计划重大项目(2019-01-07-00-07-E00073)。
