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Covalent Proximity Inducers. | LitMetric

Covalent Proximity Inducers.

Chem Rev

Department of Chemical and Structural Biology, The Weizmann Institute of Science, Rehovot 7610001, Israel.

Published: December 2024

AI Article Synopsis

Article 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.

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Source
http://dx.doi.org/10.1021/acs.chemrev.4c00570DOI Listing

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