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Molecules 2018, 23(2), 311; https://doi.org/10.3390/molecules23020311

The Road from Host-Defense Peptides to a New Generation of Antimicrobial Drugs

Instituto de Productos Naturales y Agrobiología del CSIC, CSIC-Spanish Research Council, Avda. Astrofísico Fco. Sánchez, 3-38206 La Laguna, Tenerife, Spain
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Received: 27 December 2017 / Revised: 23 January 2018 / Accepted: 30 January 2018 / Published: 1 February 2018
(This article belongs to the Special Issue Emerging Drug Discovery Approaches against Infectious Diseases)
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Abstract

Host-defense peptides, also called antimicrobial peptides (AMPs), whose protective action has been used by animals for millions of years, fulfill many requirements of the pharmaceutical industry, such as: (1) broad spectrum of activity; (2) unlike classic antibiotics, they induce very little resistance; (3) they act synergically with conventional antibiotics; (4) they neutralize endotoxins and are active in animal models. However, it is considered that many natural peptides are not suitable for drug development due to stability and biodisponibility problems, or high production costs. This review describes the efforts to overcome these problems and develop new antimicrobial drugs from these peptides or inspired by them. The discovery process of natural AMPs is discussed, as well as the development of synthetic analogs with improved pharmacological properties. The production of these compounds at acceptable costs, using different chemical and biotechnological methods, is also commented. Once these challenges are overcome, a new generation of versatile, potent and long-lasting antimicrobial drugs is expected. View Full-Text
Keywords: antimicrobial; antibiotic; peptides; AMP; cathelicidins; site-selective; peptide modification; tag-and-modify; customizable units; gene mining antimicrobial; antibiotic; peptides; AMP; cathelicidins; site-selective; peptide modification; tag-and-modify; customizable units; gene mining
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Boto, A.; Pérez de la Lastra, J.M.; González, C.C. The Road from Host-Defense Peptides to a New Generation of Antimicrobial Drugs. Molecules 2018, 23, 311.

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