Abstract
Virtually every living organism produces gene-encoded antimicrobial peptides (AMPs) that provide an immediate defence against pathogen invasion. Many AMPs have been isolated and used as antibiotics that are effective against multidrug-resistant bacteria. Although encouraging, AMPs have such poor drug-like properties that their application for clinical use is restricted. In turn, this has diverted research to the development of synthetic molecules that retain the therapeutic efficacy of AMPs but are endowed with greater biological stability and safety profiles. Most of the synthetic molecules, either based on a peptidic or non-peptidic scaffold, have been designed to mimic the amphiphilic properties of native AMPs, which are widely believed to be the key determinant of their antibacterial activity. In this review, the structural, chemical and biophysical features that govern the biological activities of various synthetic designs are discussed extensively. Recent innovative approaches from the literature that exhibit novel concepts towards the development of new synthetic antibacterial agents, including the engineered delivery platform incorporated with AMP mimetics, are also emphasised.
Keywords: Antimicrobial peptides, synthetic mimics, antibacterial, amphiphilic properties, multidrug-resistant bacteria, peptide, polymer, peptidomimetics.
Current Medicinal Chemistry
Title:Towards the Development of Synthetic Antibiotics: Designs Inspired by Natural Antimicrobial Peptides
Volume: 23 Issue: 41
Author(s): Fazren Azmi, Mariusz Skwarczynski and Istvan Toth
Affiliation:
Keywords: Antimicrobial peptides, synthetic mimics, antibacterial, amphiphilic properties, multidrug-resistant bacteria, peptide, polymer, peptidomimetics.
Abstract: Virtually every living organism produces gene-encoded antimicrobial peptides (AMPs) that provide an immediate defence against pathogen invasion. Many AMPs have been isolated and used as antibiotics that are effective against multidrug-resistant bacteria. Although encouraging, AMPs have such poor drug-like properties that their application for clinical use is restricted. In turn, this has diverted research to the development of synthetic molecules that retain the therapeutic efficacy of AMPs but are endowed with greater biological stability and safety profiles. Most of the synthetic molecules, either based on a peptidic or non-peptidic scaffold, have been designed to mimic the amphiphilic properties of native AMPs, which are widely believed to be the key determinant of their antibacterial activity. In this review, the structural, chemical and biophysical features that govern the biological activities of various synthetic designs are discussed extensively. Recent innovative approaches from the literature that exhibit novel concepts towards the development of new synthetic antibacterial agents, including the engineered delivery platform incorporated with AMP mimetics, are also emphasised.
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Cite this article as:
Azmi Fazren, Skwarczynski Mariusz and Toth Istvan, Towards the Development of Synthetic Antibiotics: Designs Inspired by Natural Antimicrobial Peptides, Current Medicinal Chemistry 2016; 23 (41) . https://dx.doi.org/10.2174/0929867323666160825162435
DOI https://dx.doi.org/10.2174/0929867323666160825162435 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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