Novel insights into histone lysine methyltransferases in cancer therapy:From epigenetic regulation to selective drugs  

作　　者：Qili Liao Jie Yang Shengfang Ge Peiwei Chai Jiayan Fan Renbing Jia 

机构地区：[1]Department of Ophthalmology,Ninth People's Hospital,Shanghai Jiao Tong University School of Medicine,Shanghai,200001,China [2]Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology,Shanghai,200001,China

出　　处：《Journal of Pharmaceutical Analysis》2023年第2期127-141,共15页药物分析学报（英文版）

基　　金：the Science and Technology Commission of Shanghai,China(Grant Nos.:20DZ2270800 and 19JC1410200);Innovative Research Team of High-Level Local Universities in Shanghai,China(Grant No.:SHSMU-ZDCX20210900);the National Natural Science Foundation of China(Grant No.:82073889).

摘　　要：The reversible and precise temporal and spatial regulation of histone lysine methyltransferases(KMTs)is essential for epigenome homeostasis.The dysregulation of KMTs is associated with tumor initiation,metastasis,chemoresistance,invasiveness,and the immune microenvironment.Therapeutically,their promising effects are being evaluated in diversified preclinical and clinical trials,demonstrating encouraging outcomes in multiple malignancies.In this review,we have updated recent understandings of KMTs'functions and the development of their targeted inhibitors.First,we provide an updated overview of the regulatory roles of several KMT activities in oncogenesis,tumor suppression,and immune regulation.In addition,we summarize the current targeting strategies in different cancer types and multiple ongoing clinical trials of combination therapies with KMT inhibitors.In summary,we endeavor to depict the regulation of KMT-mediated epigenetic landscape and provide potential epigenetic targets in the treatment of cancers.

关 键 词：Cancer EPIGENETICS Histone lysine methyltransferase Epigenetic inhibitors Combined therapeutic strategy Clinical application 

分 类 号：TB383.1[一般工业技术—材料科学与工程] R730.5[医药卫生—肿瘤]