BioCentury
ARTICLE | Distillery Therapeutics

Therapeutics: K-Ras (KRAS); son of sevenless homolog 1 (SOS1)

February 12, 2015 8:00 AM UTC

In vitro studies have identified stapled peptide-based inhibitors of KRAS that could help treat cancer. In a KRAS binding assay, a stapled peptide based on the α-helix of SOS1 bound wild-type and mutant KRAS with EC50 values of 106-175 nM. In a panel of cultured human cancer cell lines expressing wild-type or mutant KRAS, the stapled peptide decreased viability compared with an inactive control peptide. Next steps could include evaluating the lead SOS1-based stapled peptide in animal models of KRAS-driven cancers...