Discovery & Development of Small-Molecule Glue Degraders of KRAS G12D as the First-in-Class Anticancer Drugs
Time: 2:00 pm
day: Bootcamp Day
Details:
- Cancer cell-based drug screening identified hit compounds that abide Lipinski rule and degrade active GTP KRAS G12D protein in KRAS G12D mutated cancer cells
- High-throughput technologies revealed a novel E3 ligase and mechanism of drug action in which degraders bind the E3 ligase and KRAS G12D and induce the KRAS degradation
- Protein structure-guided and AI-powered drug design speeded up hit to lead optimization for identification of preclinical candidates as the first-in-class anticancer drugs
