ArticleRSC chemical biology2026
A new 4-atom linker enables PROTAC development and imaging.
Article in RSC chemical biology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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10 authors.
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Abstract
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional molecules, emerging as a promising class of drugs. Amongst their structural components, the linker moiety plays a pivotal role in modulating their biological activity and physicochemical properties. Current PROTAC design strategies involve utilising shorter and more rigid linkers to limit the number of possible conformations within the ternary complex. We hypothesised that employing a short diyne spacer as the linker between the two ligands could generate highly potent PROTACs. Here, we report a series of diyne-bearing, low nanomolar BRD4 degraders recruiting the CRL4
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