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Covalent Proximity Inducers

Research output: Contribution to journalReview articlepeer-review

Abstract

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.

Original languageEnglish
Pages (from-to)326-368
Number of pages43
JournalChemical Reviews
Volume125
Issue number1
DOIs
StatePublished Online - 18 Dec 2024

All Science Journal Classification (ASJC) codes

  • General Chemistry

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