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http://hdl.handle.net/2445/66210
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DC Field | Value | Language |
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dc.contributor.author | Rabanal Anglada, Francesc | - |
dc.contributor.author | Grau Campistany, Ariadna | - |
dc.contributor.author | Vila Farrés, Xavier | - |
dc.contributor.author | González-Linares, J. (Javier) | - |
dc.contributor.author | Borràs Suárez, Miquel | - |
dc.contributor.author | Vila Estapé, Jordi | - |
dc.contributor.author | Manresa Presas, Ma. Ángeles (María Ángeles) | - |
dc.contributor.author | Cajal Visa, Yolanda | - |
dc.date.accessioned | 2015-07-07T12:44:06Z | - |
dc.date.available | 2015-07-07T12:44:06Z | - |
dc.date.issued | 2015-05-29 | - |
dc.identifier.issn | 2045-2322 | - |
dc.identifier.uri | http://hdl.handle.net/2445/66210 | - |
dc.description.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. | - |
dc.format.extent | 11 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Nature Publishing Group | - |
dc.relation.isformatof | Reproducció del document publicat a: http://dx.doi.org/10.1038/srep10558 | - |
dc.relation.ispartof | Scientific Reports, 2015, vol. 5, p. 10558 | - |
dc.relation.uri | http://dx.doi.org/10.1038/srep10558 | - |
dc.rights | cc-by-nc-nd (c) Rabanal Anglada, Francesc et al., 2015 | - |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/3.0/es | - |
dc.source | Articles publicats en revistes (Biologia, Sanitat i Medi Ambient) | - |
dc.subject.classification | Desenvolupament de medicaments | - |
dc.subject.classification | Membranes (Biologia) | - |
dc.subject.classification | Pèptids | - |
dc.subject.classification | Toxicitat dels medicaments | - |
dc.subject.classification | Antibiòtics | - |
dc.subject.classification | Bacteris patògens | - |
dc.subject.other | Drug development | - |
dc.subject.other | Membranes (Biology) | - |
dc.subject.other | Peptides | - |
dc.subject.other | Drug toxicity | - |
dc.subject.other | Antibiotics | - |
dc.subject.other | Pathogenic bacteria | - |
dc.title | A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/publishedVersion | - |
dc.identifier.idgrec | 651905 | - |
dc.date.updated | 2015-07-07T12:44:06Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
dc.identifier.pmid | 26024044 | - |
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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651905.pdf | 893.07 kB | Adobe PDF | View/Open |
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