Affiliation:
1. Department of Pharmacy, School of Medicine, University of Naples ‘Federico II’, Via Domenico Montesano 49, 80131 Naples, Italy
2. Department of Agricultural Sciences, University of Naples ‘Federico II’, Via dell’ Università 100, 80055 Portici, Italy
Abstract
Antimicrobial peptides (AMPs) have recently gained attention as a viable solution for combatting antibiotic resistance due to their numerous advantages, including their broad-spectrum activity, low propensity for inducing resistance, and low cytotoxicity. Unfortunately, their clinical application is limited due to their short half-life and susceptibility to proteolytic cleavage by serum proteases. Indeed, several chemical strategies, such as peptide cyclization, N-methylation, PEGylation, glycosylation, and lipidation, are widely used for overcoming these issues. This review describes how lipidation and glycosylation are commonly used to increase AMPs’ efficacy and engineer novel AMP-based delivery systems. The glycosylation of AMPs, which involves the conjugation of sugar moieties such as glucose and N-acetyl galactosamine, modulates their pharmacokinetic and pharmacodynamic properties, improves their antimicrobial activity, and reduces their interaction with mammalian cells, thereby increasing selectivity toward bacterial membranes. In the same way, lipidation of AMPs, which involves the covalent addition of fatty acids, has a significant impact on their therapeutic index by influencing their physicochemical properties and interaction with bacterial and mammalian membranes. This review highlights the possibility of using glycosylation and lipidation strategies to increase the efficacy and activity of conventional AMPs.
Subject
Drug Discovery,Pharmaceutical Science,Molecular Medicine
Reference115 articles.
1. Antibiotic resistance;Frieri;J. Infect. Public Health,2017
2. A Review on Antibiotic Resistance: Alarm Bells are Ringing;Zaman;Cureus,2017
3. Mechanisms of Antimicrobial Resistance in ESKAPE Pathogens;Santajit;BioMed Res. Int.,2016
4. Clinical relevance of the ESKAPE pathogens;Pendleton;Expert Rev. Anti Infect. Ther.,2013
5. Antimicrobial peptides;Bahar;Pharmaceuticals,2013
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