Issue 88, 2021

Advances on chemically modified antimicrobial peptides for generating peptide antibiotics

Abstract

Antimicrobial peptides (AMPs) are pinpointed as promising molecules against antibiotic-resistant bacterial infections. Nevertheless, there is a discrepancy between the AMP sequences generated and the tangible outcomes in clinical trials. AMPs’ limitations include enzymatic degradation, chemical/physical instability and toxicity toward healthy human cells. These factors compromise AMPs’ bioavailability, resulting in limited therapeutic potential. To overcome such obstacles, peptidomimetic approaches, including glycosylation, PEGylation, lipidation, cyclization, grafting, D-amino acid insertion, stapling and dendrimers are promising strategies to fine-tune AMPs. Here we focused on chemical modifications applied for AMP optimization and how they have helped these peptide-based antibiotic candidates' design and translational potential.

Graphical abstract: Advances on chemically modified antimicrobial peptides for generating peptide antibiotics

Article information

Article type
Highlight
Submitted
14 Jul 2021
Accepted
05 Oct 2021
First published
05 Oct 2021

Chem. Commun., 2021,57, 11578-11590

Advances on chemically modified antimicrobial peptides for generating peptide antibiotics

S. B. Rezende, K. G. N. Oshiro, N. G. O. Júnior, O. L. Franco and M. H. Cardoso, Chem. Commun., 2021, 57, 11578 DOI: 10.1039/D1CC03793E

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