Investigating Penetration and Antimicrobial Activity of Vector-Bicycle Conjugates.

ABSTRACT: Growing antibiotic resistance is rapidly threatening the efficacy of treatments for Gram-negative infections. Bicycle molecules, constrained bicyclic peptides from diverse libraries generated by bacteriophage display that bind with high affinity to a chosen target are a potential new class of antibiotics. The generally impermeable bacterial outer membrane currently limits the access of peptides to bacteria. The conjugation of membrane active peptides offers an avenue for outer membrane penetration. Here, we investigate which physicochemical properties of a specific membrane active peptide (MAP), derived from ixosin-B, could be tweaked to enhance the penetration of conjugates by generating multiple MAP-Bicycle conjugate variants. We demonstrate that charge and hydrophobicity are important f

SUBMITTER: Hadjicharalambous A 

PROVIDER: S-EPMC11249977 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature