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用小分子和双功能的分子准核糖酶

Lydia Borgelt^1,2, Peng Wu^1,2

¹Chemical Genomics Centre, Max Planck Institute of Molecular Physiology, Otto-Hahn-Str. 11, Dortmund 44227, Germany.

ACS chemical biology

|June 29, 2023

概括

针对核糖核酶 (RNases) 的小分子通过调节RNA生物学来提供治疗潜力. 最近的进展包括用于向RNA降解或处理抑制的双功能分子,扩大治疗应用.

科学领域:

生物化学生物化学
分子生物学分子生物学
化学生物学化学生物学

背景情况:

核糖酶 (RNases) 是关键的酶,可以分裂和处理RNA分子.
RNase活动调节RNA生物发生,新陈代谢和降解,影响细胞功能.
RNases是各种疾病的有效治疗标,包括感染,自身免疫性疾病和癌症.

研究的目的:

总结发现小分子抑制剂和激活剂的发现,这些激活剂针对细菌,病毒和人类RNases.
要突出新兴的双功能分子,利用化学诱导的接近性来进行基于RNase的RNA操纵.
讨论目前的趋势和发展RNase向分子的未来前景,用于生物和治疗应用.

主要方法:

针对RNases的小分子发现工作的文献综述.
对RNase调节的化学诱导近距离策略的最新进展进行分析.
设计用于RNase介导的RNA降解或加工抑制的双功能分子的合成和表征.

主要成果:

已经确定了各种RNase的许多小分子抑制剂和激活剂.
双功能分子展示了精确向和降解RNA的新机制.
新兴的战略显示出开发针对性治疗针对异常RNA代谢驱动的疾病的前景.

结论:

针对RNase的小分子代表了治疗干预的有希望的途径.
双功能分子在调节RNA生物学方面提供了增强的特异性和有效性.
对RNase向剂的持续开发具有各种临床应用的巨大潜力.

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