Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders
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https://figshare.com/articles/dataset/Potent_and_Preferential_Degradation_of_CDK6_via_Proteolysis_Targeting_Chimera_Degraders/9236537
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资源简介：
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.
创建时间：
2019-07-22
