靶向HBV cccDNA生成和转录的小分子调控剂研究进展  

Advances in research on small molecule regulators targeting HBV cccDNA generation and transcription

作　　者：徐祥瑞 金昱 徐淑静 王硕 何勇 刘新泳[1] 展鹏[1] XU Xiang-rui;JIN Yu;XU Shu-jing;WANG Shuo;HE Yong;LIU Xin-yong;ZHAN Peng(Department of Medicinal Chemistry,School of Pharmaceutical Sciences,Shandong University,Jinan 250012,China)

机构地区：[1]山东大学药学院,药物化学研究所,山东济南250012

出　　处：《药学学报》2023年第10期2979-2994,共16页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金面上项目(82173677);山东省杰出青年基金(ZR2020JQ31)。

摘　　要：乙型肝炎病毒(hepatitis B virus,HBV)对人类生命健康造成严重危害。虽然目前已有多种治疗乙肝的上市药物,但由于共价闭合环状DNA(covalently closed circular DNA,cccDNA)的持续存在,导致出现停药后容易复发的问题,这也是乙肝难以治愈的根源。本文对cccDNA生成、转录和复制的调控机制进行综述,并从药物化学的视角对相关小分子调控剂的研究进展进行了总结。Hepatitis B virus(HBV)represents a significant global public health challenge.Despite the availability of several approved drugs for hepatitis B treatment,the persistence of covalently closed circular DNA(cccDNA)renders HBV eradication elusive,thereby leading to disease relapse after drug withdrawal.This paper reviews the regulatory mechanisms of cccDNA formation,transcription and replication,and summarizes the research progress of related small molecule regulators from the perspective of medicinal chemistry.

关 键 词：乙型肝炎病毒 共价闭合环状DNA 小分子化合物 药物化学 药物设计 

分 类 号：R914[医药卫生—药物化学]