Targeting KRAS Mutations Beyond G12C: Advancing ACBI3 for Comprehensive KRAS Degradation and Tumour Regression
Time: 1:45 pm
day: Day 1, Track 2, PM
Details:
- Addressing the challenge of undruggable KRAS mutants and secondary mutations by developing ACBI3 as a next-generation therapeutic targeting a broader range of KRAS variants
- Leveraging a fragment-first approach and structure-guided optimization to refine ACBI3 (a compound developed collaboratively by Boehringer Ingelheim and Prof. Alessio Ciulli’s group) to enhance its biophysical properties and therapeutic potential
- Demonstrating the ability of ACBI3 to selectively degrade prevalent oncogenic KRAS variants, sparing H- and NRAS, resulting in a potent reduction of KRAS signalling and tumour regression in preclinical models
