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2015-05-29

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cc-by-nc-nd (c) Rabanal Anglada, Francesc et al., 2015
Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/66210

A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity

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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.

Related resource

http://dx.doi.org/10.1038/srep10558

Subject

Desenvolupament de medicaments, Membranes (Biologia), Pèptids, Toxicitat dels medicaments, Antibiòtics, Bacteris patògens

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Drug development, Membranes (Biology), Peptides, Drug toxicity, Antibiotics, Pathogenic bacteria

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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)

Citation

RABANAL ANGLADA, Francesc, et al. A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity. Scientific Reports. 2015. Vol. 5, num. 10558. ISSN 2045-2322. [consulted: 16 of October of 2026]. Available at: https://hdl.handle.net/2445/66210

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