Development of KRAS-degrader drugs against cancer
Category: Pharmaceutical
Exhibitor: DEVELOPMENT CENTER FOR BIOTECHNOLOGY
Booth No: S212a
Characteristic
PROteolysis-Targeting Chimera (PROTAC) is one of the target protein degradation technology. Target proteins can be degraded through ubiquitin labeling and proteasome degradation. PROTAC can be applied to highly resistance targets or undruggable targets.
We apply PROTAC technology on mutated KRAS treatment. It is highly expressed in pancreatic cancer, non-small cell lung cancer and colorectal cancer. By degrading KRAS mutation protein, RAS-PROTAC may show clinical benefit on KRAS highly expressed cancers.
A series of lead compounds exhibited inhibitory effects in cell lines expressed KRAS mutation type G12C, G12D, and G12V as well as significant protein degradation. The in vivo efficacy of the lead compound was observed in NCI-H441 xenograft model with TGI > 60%.
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