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.

中文翻译：

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共价邻位诱导器


能够在两种蛋白质之间诱导接近的分子在化学生物学和药物发现中的应用越来越多。引入亲电试剂并使此类邻近诱导剂共价的能力可以提供更好的特性，例如选择性、效力、作用持续时间和减小的分子大小。这个概念在靶向降解的背景下已经被大量探索，特别是对于二价分子，但最近，在其他环境中以及一价分子胶中也有其他应用报道。这是对已报道的共价邻位诱导剂的全面综述，旨在确定其发现和应用中的常见趋势和当前差距。