Please use this identifier to cite or link to this item:
http://hdl.handle.net/2445/66210
Title: | A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity |
Author: | Rabanal Anglada, Francesc Grau Campistany, Ariadna Vila Farrés, Xavier González-Linares, J. (Javier) Borràs Suárez, Miquel Vila Estapé, Jordi Manresa Presas, Ma. Ángeles (María Ángeles) Cajal Visa, Yolanda |
Keywords: | Desenvolupament de medicaments Membranes (Biologia) Pèptids Toxicitat dels medicaments Antibiòtics Bacteris patògens Drug development Membranes (Biology) Peptides Drug toxicity Antibiotics Pathogenic bacteria |
Issue Date: | 29-May-2015 |
Publisher: | Nature Publishing Group |
Abstract: | Bacterial resistance to almost all available antibiotics is an important public health issue. A major goal in antimicrobial drug discovery is the generation of new chemicals capable of killing pathogens with high selectivity, particularly multi-drug-resistant ones. Here we report the design, preparation and activity of new compounds based on a tunable, chemically accessible and upscalable lipopeptide scaffold amenable to suitable hit-to-lead development. Such compounds could become therapeutic candidates and future antibiotics available on the market. The compounds are cyclic, contain two D-amino acids for in vivo stability and their structures are reminiscent of other cyclic disulfide-containing peptides available on the market. The optimized compounds prove to be highly active against clinically relevant Gram-negative and Gram-positive bacteria. In vitro and in vivo tests show the low toxicity of the compounds. Their antimicrobial activity against resistant and multidrug-resistant bacteria is at the membrane level, although other targets may also be involved depending on the bacterial strain. |
Note: | Reproducció del document publicat a: http://dx.doi.org/10.1038/srep10558 |
It is part of: | Scientific Reports, 2015, vol. 5, p. 10558 |
URI: | http://hdl.handle.net/2445/66210 |
Related resource: | http://dx.doi.org/10.1038/srep10558 |
ISSN: | 2045-2322 |
Appears in Collections: | Articles publicats en revistes (Biologia, Sanitat i Medi Ambient) Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica) Articles publicats en revistes (Fonaments Clínics) Articles publicats en revistes (Química Inorgànica i Orgànica) |
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