Capitalizing on Structural Biology to Target the Oncogenic State of RAS Mutants with RAS(ON) Tri-Complex Inhibitors
Time: 11:45 am
day: Day 2
Details:
- Exploring the rational design of a natural product-inspired small molecule created a neomorphic surface on an intracellular chaperone cyclophilin A that was exploited to target active KRASG12C with high affinity and selectivity
- Harnessing further structure-guided optimization to design a novel, non-covalent compound with broad activity across the active state of multiple oncogenic (H/K/N) RAS variants
- Showcasing the preclinical data to demonstrate the Tri-complex inhibitors selectively target active KRASG12C or multiple RAS mutants and are now in clinical trials
