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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)
Toxicitat dels medicaments
Bacteris patògens
Drug development
Membranes (Biology)
Drug toxicity
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.
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It is part of: Scientific Reports, 2015, vol. 5, p. 10558
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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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