合成抗生素的发展：天然抗菌肽设计

Title:Towards the Development of Synthetic Antibiotics: Designs Inspired by Natural Antimicrobial Peptides

Volume: 23 Issue: 41

Author(s): Fazren Azmi, Mariusz Skwarczynski, Istvan Toth

Affiliation:

关键词: 抗菌肽，合成的模仿，抗菌，两亲性，多重耐药菌、肽、肽聚合物。

摘要: 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.

Cite this article as:

Fazren Azmi, Mariusz Skwarczynski, Istvan Toth , 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