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基于多向药理学的BET Bromodomain抑制剂及降解剂研究进展
引用本文:陈红丽,陈海芳,张智敏,陆涛,陈亚东.基于多向药理学的BET Bromodomain抑制剂及降解剂研究进展[J].国际药学研究杂志,2017,44(6).
作者姓名:陈红丽  陈海芳  张智敏  陆涛  陈亚东
作者单位:1. 211198,南京 中国药科大学理学院;2. 310003,杭州 浙江省 医学科学院药物研究所
基金项目:国家自然科学基金资助项目,江苏省高校"青蓝工程"资助项目
摘    要:溴结构域和末端外结构域(BET)Bromodomain已成为可用于治疗癌症和其他人类疾病的新靶标.目前已发现了几类有效的选择性小分子BET Bromodomain抑制剂,且多种已处于临床开发中.临床前和临床数据已证明BET Bromodomain抑制剂有良好的前景,但也存在耐药性等潜在缺陷.目前人们正在尝试将具有不同作用机制的靶标与BET Bromodomain组合,开发基于多向药理学的BET Bromodomain抑制剂及降解剂.本文综述了激酶/BET小分子抑制剂、组蛋白去乙酰化酶/BET小分子抑制剂及BET蛋白降解剂,为后续针对BET蛋白更深入的研究提供思路.

关 键 词:溴结构域和末端外结构域  Bromodomain  多向药理学  小分子抑制剂  蛋白降解剂

BET Bromodomain inhibitors and degraders based on polypharmacology:research advances
CHEN Hong-li,CHEN Hai-fang,ZHANG Zhi-min,LU Tao,CHEN Ya-dong.BET Bromodomain inhibitors and degraders based on polypharmacology:research advances[J].Foreign Medical Sciences(Section of Pharmarcy),2017,44(6).
Authors:CHEN Hong-li  CHEN Hai-fang  ZHANG Zhi-min  LU Tao  CHEN Ya-dong
Abstract:Bromodomain and extra-terminal domain(BET)Bromodomain has become a new target for the treatment of cancers and other human disorders. Nowadays,several classes of its potent and selective small-molecule inhibitors have been identified,many of which are in clinical trials. Preclinical and clinical data have shown that BET Bromodomain inhibitors have good prospects. Howev-er,there are potential therapeutic deficiencies,such as drug resistance. At present,attempts are being made to develop BET Bromodo-main inhibitors and degraders based on polypharmacology,combining BET Bromodomain with other targets of different mechanisms. In this paper,small-molecule kinase/BET inhibitors,small-molecule histone deacetylases(HDAC)/BET inhibitors and BET protein degraders are reviewed,which may provide guidance for further research on BET protein.
Keywords:Bromodomain and extra-terminal domain(BET)  Bromodomain  polypharmacology  small-molecule inhibitors  protein degraders
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