Document Report Card

ID: ALA1145752

Journal: J Med Chem

Title: Dissociation of antibacterial and hemolytic activities of an amphipathic peptide antibiotic.

Authors: Qin C, Zhong X, Bu X, Ng NL, Guo Z.

Abstract: Using an alanine-scanning method, we have found that the antibacterial and hemolytic activities of the amphipathic cyclic decapeptide antibiotic tyrocidine A depend on different structural components. Single substitution of glutamine-6 of the natural product with a cationic amino acid results in a therapeutic index enhancement of up to 140-fold. Successful dissociation of the two intimately associated properties should enable discovery of novel analogues with both high bacterial selectivity and antibacterial potency to counter microbial resistance.

CiteXplore: 14584933

DOI: 10.1021/jm0341352