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Updated: Jan 21, 2026

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
Published on: November 9, 2020
Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders
Shang Su1, Zimo Yang2, Hongying Gao1,2
1MOE Key Laboratory of Protein Sciences, School of Life Sciences , Tsinghua University , Beijing 100084 , P. R. China.
Abstract:
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 proliferation of hematopoietic cancer cells including multiple myeloma and robustly degraded copy-amplified/mutated forms of CDK6, indicating future potential clinical applications.
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