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dc.contributor.authorHernando Santa Cruz, Elsa 
dc.contributor.authorCapurro, Valeria
dc.contributor.authorCossu, Claudia .
dc.contributor.authorFiore, Michele .
dc.contributor.authorGarcía Valverde, María 
dc.contributor.authorSoto Cerrato, Vanessa
dc.contributor.authorPérez Tomás, Ricardo
dc.contributor.authorMoran, Oscar .
dc.contributor.authorZegarra Moran, Olga .
dc.contributor.authorQuesada Pato, Roberto 
dc.date.accessioned2018-08-21T08:54:14Z
dc.date.available2018-08-21T08:54:14Z
dc.date.issued2018-02
dc.identifier.issn2045-2322
dc.identifier.urihttp://hdl.handle.net/10259/4873
dc.description.abstractAnion selective ionophores, anionophores, are small molecules capable of facilitating the transmembrane transport of anions. Inspired in the structure of natural product prodigiosin, four novel anionophores 1a-d, including a 1,2,3-triazole group, were prepared. These compounds proved highly efficient anion exchangers in model phospholipid liposomes. The changes in the hydrogen bond cleft modified the anion transport selectivity exhibited by these compounds compared to prodigiosin and suppressed the characteristic high toxicity of the natural product. Their activity as anionophores in living cells was studied and chloride efflux and iodine influx from living cells mediated by these derivatives was demonstrated. These compounds were shown to permeabilize cellular membranes to halides with efficiencies close to the natural anion channel CFTR at doses that do not compromise cellular viability. Remarkably, optimal transport efficiency was measured in the presence of pH gradients mimicking those found in the airway epithelia of Cystic Fibrosis patients. These results support the viability of developing small molecule anionophores as anion channel protein surrogates with potential applications in the treatment of conditions such as Cystic Fibrosis derived from the malfunction of natural anion transport mechanisms.en
dc.description.sponsorshipEuropean Union’s Horizon 2020 research and innovation programme under grant agreement No. 667079, La Marató de TV3 Foundation (20132730), Consejería de Educación de la Junta de Castilla y León (Projects BU340U13 and BU092U16)en
dc.format.mimetypeapplication/pdf
dc.language.isoenges
dc.publisherNature Publishing Groupen
dc.relation.ispartofScientific Reports. 2018, 8, art. 2608en
dc.rightsAttribution 4.0 International
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.subject.otherQuímica orgánicaes
dc.subject.otherChemistry, Organicen
dc.titleSmall molecule anionophores promote transmembrane anion permeation matching CFTR activityen
dc.typeArtículoes
dc.typeinfo:eu-repo/semantics/article
dc.rights.accessRightsinfo:eu-repo/semantics/openAccess
dc.relation.publisherversionhttps://doi.org/10.1038/s41598-018-20708-3
dc.identifier.doi10.1038/s41598-018-20708-3
dc.relation.projectIDinfo:eu-repo/grantAgreement/EC/H2020/667079
dc.relation.projectIDinfo:eu-repo/grantAgreement/TV3Foundation/20132730
dc.relation.projectIDinfo:eu-repo/grantAgreement/JCyL/BU340U13
dc.relation.projectIDinfo:eu-repo/grantAgreement/JCyL/BU092U16
dc.type.hasVersioninfo:eu-repo/semantics/publishedVersionen


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