组蛋白修饰抑制剂在转移性去势抵抗性前列腺癌中的研究进展  

Research progress of histone modification inhibitors in treatment of metastatic castration-resistant prostate cancer

作　　者：叶世杰 黄瑞达 周旋 孟祥余 王科洁 马琪 YE Shi-jie;HUANG Rui-da;ZHOU Xuan;MENG Xiang-yu;WANG Ke-jie;MA Qi(Health Science Center,Ningbo University,Ningbo ZHEJIANG 315211,China;Department of Pharmacy,the First Affiliated Hospital of Ningbo University,Ningbo ZHEJIANG 315010,China;Translational Research Laboratory for Urology,the First Affiliated Hospital of Ningbo University,Ningbo ZHEJIANG 315010,China;Comprehensive Genitourinary Cancer Center,the First Affiliated Hospital of Ningbo University,Ningbo ZHEJIANG 315010,China;Zhejiang Engineering Research Center of Innovative Technologies and Diagnostic and Therapeutic Equipment for Urinary Systerm Diseases,the First Affiliated Hospital of Ningbo University,Ningbo ZHEJIANG 315010,China)

机构地区：[1]宁波大学医学部,浙江宁波315211 [2]宁波大学附属第一医院药学部 [3]宁波大学附属第一医院泌尿系统疾病转化医学研究重点实验室,浙江宁波315010 [4]宁波大学附属第一医院泌尿肿瘤综合诊治中心,浙江宁波315010 [5]宁波大学附属第一医院泌尿系统疾病创新技术与诊疗器械浙江省工程研究中心,浙江宁波315010

出　　处：《中国新药与临床杂志》2025年第3期181-188,共8页Chinese Journal of New Drugs and Clinical Remedies

基　　金：宁波市自然科学基金项目(2021J259)。

摘　　要：转移性去势抵抗性前列腺癌(mCRPC)在前列腺癌治疗中仍具挑战性。近年来研究表明组蛋白修饰异常在mCRPC的发展过程中起到重要作用,目前已有多种组蛋白修饰抑制剂应用于mCRPC的治疗研究中,并有可能成为未来mCRPC的治疗策略之一。本文综述了组蛋白甲基化与乙酰化修饰在mCRPC进程中的作用机制,并介绍了组蛋白甲基化与去甲基化抑制剂、乙酰化与去乙酰化抑制剂以及溴结构域和超末端结构域蛋白抑制剂在mCRPC中的研究进展。Metastatic castration-resistant prostate cancer(mCRPC)remains a challenge in the treatment of prostate cancer.In recent years,with the understanding of histone modification,it has been found that histone modification may become a new therapeutic target for mCRPC.At present,a large number of basic and clinical studies have shown that histone modification inhibitors may improve the prognosis of mCRPC patients.This article reviewed the mechanisms of histone methylation and acetylation in mCRPC,and introduced the potential application value of histone methylation and demethylation inhibitors,acetylation and deacetylation inhibitors,and bromodomain and extra-terminal domain inhibitors in mCRPC,providing a scientific basis for the possibility of histone modification inhibitors as a new strategy for the treatment of mCRPC.

关 键 词：表观遗传学 转移性去势抵抗性前列腺癌 组蛋白修饰 甲基化 乙酰化 

分 类 号：R737[医药卫生—肿瘤]