Gramicidin A-based unimolecular channel: cancer cell-targeting behavior and ion transport-induced apoptosis

Abstract

A series of glycoside–peptide conjugates were prepared by engineering at the N-terminus of the natural peptide gramicidin A. The conjugate containing galactose moiety formed a unimolecular transmembrane channel and mediated ion transport to induce apoptosis of cancer cells. More importantly, it exhibited liver cancer cell-targeting behavior due to the galactose–asialoglycoprotein receptor recognition.