Development of PROTAC degrader probe of CDK4/6 based on DCAF16

Chunlan Pu,Yuanyuan Liu,Rui Deng,Qingjia Xu,Shirui Wang,Hongjia Zhang,Dan Luo,Xinyu Ma,Yu Tong,Rui Li

Bioorganic Chemistry（2023）

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摘要

•Compound A4 is an efficient DCAF16-based PROTACs that induces the degradation of CDK4/6.•Compound A4 exhibits 7 times lower toxicity than Palbociclib in non-tumor cells LO2.•Compound A4 capable of achieving antitumor activity in TNBC cell lines MDA-MB-231 both in vitro and in vivo.

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protac degrader probe,dcaf16

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