药学研究2024,Vol.43Issue(1) :83-88.DOI:10.13506/j.cnki.jpr.2024.01.015

靶向转录因子的抗肿瘤药物研发进展

Research and development progress of anti-tumor drug targeting transcription factors

路明英 胡唯伟 高兴华
药学研究2024,Vol.43Issue(1) :83-88.DOI:10.13506/j.cnki.jpr.2024.01.015

靶向转录因子的抗肿瘤药物研发进展

Research and development progress of anti-tumor drug targeting transcription factors

路明英 1胡唯伟 1高兴华1
扫码查看

作者信息

  • 1. 中国药科大学,江苏南京 211198
  • 折叠

摘要

转录因子(transcription factor,TF)通过与DNA链上特定结合位点的结合,转录调控信号通路中不同蛋白的表达,进而参与调控多种细胞的正常生理过程,如细胞增殖、代谢、凋亡、免疫反应和分化等.TFs的异常表达促进了肿瘤的发生发展,以TFs为靶点成为药物研发的新思路.然而,结构紊乱和结合口袋的缺乏使得靶向TFs的药物设计具有挑战性.本综述将总结靶向TFs的小分子药物开发研究进展以及一些已经取得成功的案例,以证明靶向TFs成药的可行性.

Abstract

Transcription factor(TF)control many normal cellular processes such as cell growth and proliferation,me-tabolism,apoptosis,immune response and differentiation by binding to DNA-regulatory sequences.TFs are often dysregulated in cancer and associate with initiation and progression of cancer.Therefore targeting TFs provides new ideas for the development of anticancer drugs.However,drug design targeting TFs faces challenges because of structural disorder and lack of binding pockets.This review was focused on the advances and successes in the development of small molecules targe-ting TFs and demonstrates feasibility of drug discovery targeting TFs and provides paradigms for the development of drugs targeting TFs.

关键词

转录因子/抑制剂/TF-DNA相互作用/蛋白-蛋白相互作用/PROTAC

Key words

TF/Inhibitors/TF-DNA interaction/Protein-protein interaction/PROTAC

引用本文复制引用

基金项目

国家自然科学基金(82073280)

出版年

2024
药学研究
山东省药品检验所 山东省药学会

药学研究

CSTPCD
影响因子:0.653
ISSN:2095-5375
参考文献量47
段落导航相关论文