共价接近诱导剂

IF 51.4 1区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Chemical Reviews Pub Date : 2024-12-18 DOI:10.1021/acs.chemrev.4c00570
Nir London
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引用次数: 0

摘要

能够诱导两种蛋白质之间接近的分子在化学生物学和药物发现中得到越来越多的应用。引入亲电试剂并使这种接近诱导剂共价的能力可以提供诸如选择性、效力、作用持续时间和减小分子尺寸等改进的特性。这个概念已经在靶向降解的背景下进行了大量的探索,特别是对于二价分子,但最近,在其他背景下的其他应用被报道,以及单价分子胶。这是一个全面的审查报告共价接近诱导剂,旨在确定其发现和应用的共同趋势和目前的差距。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Covalent Proximity Inducers
Molecules that are able to induce proximity between two proteins are finding ever increasing applications in chemical biology and drug discovery. The ability to introduce an electrophile and make such proximity inducers covalent can offer improved properties such as selectivity, potency, duration of action, and reduced molecular size. This concept has been heavily explored in the context of targeted degradation in particular for bivalent molecules, but recently, additional applications are reported in other contexts, as well as for monovalent molecular glues. This is a comprehensive review of reported covalent proximity inducers, aiming to identify common trends and current gaps in their discovery and application.
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来源期刊
Chemical Reviews
Chemical Reviews 化学-化学综合
CiteScore
106.00
自引率
1.10%
发文量
278
审稿时长
4.3 months
期刊介绍: Chemical Reviews is a highly regarded and highest-ranked journal covering the general topic of chemistry. Its mission is to provide comprehensive, authoritative, critical, and readable reviews of important recent research in organic, inorganic, physical, analytical, theoretical, and biological chemistry. Since 1985, Chemical Reviews has also published periodic thematic issues that focus on a single theme or direction of emerging research.
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