Targeting epigenetic regulators to overcome drug resistance in cancers  

作　　者：Nan Wang Ting Ma Bin Yu 

机构地区：[1]Institute of Drug Discovery&Development,School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001,China

出　　处：《Signal Transduction and Targeted Therapy》2023年第3期1070-1093,共24页信号转导与靶向治疗（英文）

基　　金：This work is supported by the National Natural Science Foundation of China(nos.22277110,81973177,and 81903770);Natural Science Foundation of Henan Province(no.222300420069);Program for Science&Technology Innovation Talents in Universities of Henan Province(no.21HASTIT045);Key scientific and technological projects of Henan Province(no.222102310125);China Postdoctoral Science Foundation(No.2019M662556).

摘　　要：Drug resistance is mainly responsible for cancer recurrence and poor prognosis.Epigenetic regulation is a heritable change in gene expressions independent of nucleotide sequence changes.As the common epigenetic regulation mechanisms,DNA methylation,histone modification,and non-coding RNA regulation have been well studied.Increasing evidence has shown that aberrant epigenetic regulations contribute to tumor resistance.Therefore,targeting epigenetic regulators represents an effective strategy to reverse drug resistance.In this review,we mainly summarize the roles of epigenetic regulation in tumor resistance.In addition,as the essential factors for epigenetic modifications,histone demethylases mediate the histone or genomic DNA modifications.Herein,we comprehensively describe the functions of the histone demethylase family including the lysine-specific demethylase family,the Jumonji C-domain-containing demethylase family,and the histone arginine demethylase family,and fully discuss their regulatory mechanisms related to cancer drug resistance.In addition,therapeutic strategies,including small-molecule inhibitors and small interfering RNA targeting histone demethylases to overcome drug resistance,are also described.

关 键 词：EPIGENETIC drug OVERCOME 

分 类 号：R392.2[医药卫生—免疫学]