针对表观遗传阅读器"BET"作为癌症治疗策略
Abhishek Wahi1, Namish Manchanda1, Priti Jain1
1Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Delhi Pharmaceutical Sciences and Research University, Govt. of NCT of Delhi, Delhi, New Delhi 110017, India.
Bioorganic chemistry
|September 8, 2023
概括
原体和额外终端 (BET) 蛋白调节参与癌症的基因. BET 抑制剂显示出有希望但有局限性,推动了选择性抑制剂的研究,以改善癌症治疗,减少副作用.
科学领域:
- 表观遗传学 在表观遗传学中,表观遗传学是指表观遗传学.
- 分子生物学分子生物学
- 在瘤学瘤学.
背景情况:
- 原蛋白和额外终端 (BET) 蛋白质是结合乙化氨酸残留物的表观遗传阅读器.
- BET蛋白调节基因转录,染色体动态和细胞过程,在癌症进展中发挥作用.
- 该BET家族包括BRD2,BRD3,BRD4和BRDT.
研究的目的:
- 审查BET蛋白在癌症进展中的作用.
- 讨论当前的BET抑制剂 (BETis) 和它们的局限性.
- 探索开发改进的BET抑制剂的新策略.
主要方法:
- 对BET蛋白及其抑制剂的现有文献的综述.
- 对具有泛BET活性的小分子抑制剂的分析.
- 讨论开发选择性BET抑制剂 (例如BET-BD1,BET-BD2) 的策略.
主要成果:
- BET蛋白在各种癌症的发病过程中至关重要.
- 目前的BET抑制剂在临床有效性和不良影响方面面临挑战.
- 开发异型选择性BET抑制剂是一个有前途的战略.
结论:
- 准BET蛋白是一种可行的癌症治疗方法.
- 需要新的策略来提高BET抑制剂的疗效和安全性.
- 异形选择性BET抑制剂为开发具有副作用减少的药物提供了途径.
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