EGFR(2R)-lytic peptide

EGFR(2R)-lytic peptide is a hybrid peptide therapeutic composed of an EGFR-binding peptide fragment conjugated to a lytic peptide fragment, connected by three glycine spacers. The '(2R)' designation indicates that the second amino acid of the EGFR-binding peptide fragment is arginine (R), which was modified from histidine (H) in the original EGFR-lytic peptide to improve binding affinity to EGFR. This peptide-based biologic targets the epidermal growth factor receptor (EGFR) and has demonstrated cytotoxic activity against EGFR-expressing cancer cells, including oesophageal squamous cell carcinoma (OSCC), breast cancer, pancreatic cancer, lung cancer, prostate cancer, and glioma. The peptide works by binding to EGFR on cancer cell surfaces and then disrupting the cell membrane, leading to rapid cell death. Preclinical studies have shown that EGFR(2R)-lytic peptide exhibits 1.2-1.9-fold higher cytotoxic activity compared to the original EGFR-lytic peptide and demonstrates significant antitumor activity in xenograft models at doses as low as 1 mg/kg, with no identifiable adverse effects in mice.

Other names

EGFR(2R)-lytic hybrid peptidemutated EGFR-lytic peptide