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A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity
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
Universitat de Barcelona
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.
Desenvolupament de medicaments
Membranes (Biologia)
Pèptids
Toxicitat dels medicaments
Antibiòtics
Bacteris patògens
Drug development
Membranes (Biology)
Peptides
Drug toxicity
Antibiotics
Pathogenic bacteria
cc-by-nc-nd (c) Rabanal Anglada, Francesc et al., 2015
http://creativecommons.org/licenses/by-nc-nd/3.0/es
Artículo
info:eu-repo/semantics/publishedVersion
Nature Publishing Group
         

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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
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
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
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
Grau Campistany, Ariadna; Pujol Cubells, Montserrat; Marqués Villavecchia, Ana M.; Manresa Presas, Ma. Ángeles (María Ángeles); Rabanal Anglada, Francesc; Cajal Visa, Yolanda