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针对癌症治疗的基因组脱乙酶:趋势和挑战

Tao Liang^1,2, Fengli Wang³, Reham M Elhassan²

¹Department of Pharmacy, the Second Hospital Affiliated Wannan Medical College, Wuhu 241000, China.

Acta pharmaceutica Sinica. B

|July 10, 2023

概括

基因组脱乙酶抑制剂 (HDACis) 在癌症治疗中表现有前途,但具有毒性. 本综述探讨了下一代HDAC抑制剂,包括异形选择性和多位药物,以提高疗效和减少副作用.

科学领域:

生物化学生物化学
分子生物学分子生物学
药理学药理学是指药理学的学科.

背景情况:

组织激素脱乙酶 (HDACs) 的失调与癌症的发展和进展有关.
五种HDAC抑制剂 (HDACis) 已获得批准,但传统药物会引起毒性,对固体瘤的有效性较低.
开发下一代HDAC对于改善癌症治疗至关重要.

研究的目的:

审查HDACs的生物功能和致癌作用.
探索HDAC异型的结构特征和异型选择性抑制剂的开发.
讨论用于新型抗癌策略的组合疗法,多目标药物和HDAC PROTAC.

主要方法:

对HDAC功能,瘤发生中的作用和抑制剂开发的文献综述.
分析不同HDAC异型的结构特征.
研究新兴的治疗策略,包括组合疗法,多目标药物和HDAC PROTACs.

主要成果:

HDACs在瘤发育和进展中发挥着关键作用.
目前的HDACs具有局限性,包括非目标毒性和固体瘤的低敏感性.
下一代策略,如异形选择性抑制剂,组合疗法和HDAC PROTACs,有可能提高抗癌效果,减少不良事件.

结论:

需要新型HDAC抑制剂,其异型选择性,疗效和安全性有所改善.
通过创新的方法,如多目标药物和PROTAC,向HDAC有望克服当前治疗方法的局限性.
对下一代HDAC的进一步研究可以激励开发更有效,更安全的抗癌治疗方法.

关键词:

组合疗法是一种联合疗法.这就是HDACs.多个目标的代理商.瘤发生的发生因子.这就是PROTAC.选择性抑制剂的选择性抑制剂

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