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2015-05-29

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cc-by-nc-nd (c) Rabanal Anglada, Francesc et al., 2015
Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/66210

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

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Recurs relacionat

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

Resum

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.

Matèries

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

Matèries (anglès)

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

Citació

Col·leccions

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)

Citació

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: 13 of May of 2026]. Available at: https://hdl.handle.net/2445/66210

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