cell penetrant molecular glue degrader that induce ubiquitination and degradation of cyclin K by inciting an interaction of CDK12–cyclin K with a CRL4B ligase
dCeMM2 is a cell penetrant molecular glue degrader that induce ubiquitination and degradation of cyclin K by inciting an interaction of CDK12–cyclin K with a CRL4B ligase complex. dCeMM2 induced proximity between CDK12–cyclin K and the CRL complex adaptor protein DDB1 that causes ubiquitination and proteasomal degradation of cyclin K.
Nature chemical biology, 16(11), 1199-1207 (2020-08-05)
Targeted protein degradation is a new therapeutic modality based on drugs that destabilize proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are molecular glues that can degrade otherwise unligandable proteins by orchestrating direct interactions between target
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