molecules of the month


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

Structure of (R)-CR8, a known CDK inhibitor
1 min read

(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 the molecule. This interesting mechanism is something to consider when observing unexpected cellular activities with solvent-exposed motifs in discovery programs!

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