Covalent Inhibitors of the RAS Binding Domain of PI3Kα Impair Tumor Growth Driven by RAS & HER2
- VVD designed compounds that covalently bind to cysteine 242 in the RBD of PI3K p110α and block RAS-mediated activation of PI3K activity
- These inhibitors have a profound impact on the growth of RAS-mutant and HER2 overexpressing tumors without causing hyperglycemia
- The combination of VVD compounds with other inhibitors of the RAS/MAPK pathway provides optimal efficacy in RAS-driven cancers