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Sep. 18, 2021

(R)-CR8: A CDK inhibibitor and a Molecular glue degrader of cyclin K

(R)-CR8

CDK inhib. and mol. glue degrader of cyclin K selective degradation of cyclin K in cells from characterization of 4.5k known cmpds Nature, Jun. 3, 2020 Broad Institute / Friedrich Miescher Institute

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Drug Hunter Team

( R )-CR8 is a known CDK inhibitor that was recently discovered to be a molecular glue-type degrader of cyclin K. A crystal structure of an E3 component-CR8-CDK12-cyclin K complex shows that CR8 acts by binding to the active site of a CDK (which binds to cyclin K), and recruiting an E3 component through a solvent-exposed lipophilic moiety on [...]

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