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Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders

22 Jul 2019

Abstract excerpt

A focused PROTAC library hijacking cancer therapeutic target CDK6 was developed. A design principle as "match/mismatch" was proposed for understanding the degradation profile differences in these PROTACs. Notably, potent PROTACs with specific and remarkable CDK6 degradation potential were generated by linking CDK6 inhibitor palbociclib and E3 ligase CRBN recruiter pomalidomide. The PROTAC strongly inhibited...

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PMID: 31330105
DOI: 10.1021/acs.jmedchem.9b00871

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