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Pan-KRAS Degrader
- Development stage
- Preclinical
- Lead developer
- Leadingtac
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01
Overview
Pan-KRAS Degrader is a preclinical-stage small molecule proteolysis-targeting chimera (PROTAC) being developed by Shanghai Leadingtac Pharmaceutical for the treatment of solid tumors. The compound is designed to broadly target and induce the degradation of various KRAS protein isoforms and mutants, rather than focusing on a single variant like KRAS G12C. By leveraging the cell's ubiquitin-proteasome system to eliminate the KRAS protein entirely, this "pan-degrader" approach aims to provide a more comprehensive inhibition of KRAS signaling and potentially address resistance issues encountered with traditional allele-specific KRAS inhibitors.
- Other names
- Pan-KRAS-targeted PROTAC protein degraderLeadingtac Pan-KRAS Degrader
02
Targets
KRAS (Kirsten rat sarcoma viral oncogene homolog)VHL (Von Hippel–Lindau tumor suppressor protein)
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