Article
Discovery of Novel PDEδ Degraders for the Treatment of KRAS Mutant Colorectal Cancer.
Journal of medicinal chemistry - 23 Jul 2020
Cheng Junfei, Li Yu, Wang Xu, Dong Guoqiang, Sheng Chunquan
Abstract excerpt
KRAS-PDEδ protein-protein interaction represents an appealing target for cancer therapy. However, fast release of high-affinity inhibitors from PDEδ hampered drug binding affinity and antiproliferative activity. To overcome the limitations, the first proteolysis-targeting chimeric (PROTAC) small molecules targeting PDEδ were designed. By employment of PDEδ inhibitor deltazinone (2) and cereblon ligand...
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