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Título : Small molecule anionophores promote transmembrane anion permeation matching CFTR activity
Autor : Hernando Santa Cruz, Elsa
Capurro, Valeria .
Cossu, Claudia .
Fiore, Michele .
García Valverde, María
Soto Cerrato, Vanessa .
Pérez Tomás, Ricardo .
Moran, Oscar .
Zegarra Moran, Olga .
Quesada Pato, Roberto
Publicado en: Scientific Reports. 2018, 8, art. 2608
Editorial : Nature Publishing Group
Fecha de publicación : feb-2018
ISSN : 2045-2322
DOI: 10.1038/s41598-018-20708-3
Resumen : Anion 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.
Materia: Química orgánica
Chemistry, Organic
Licencia: https://creativecommons.org/licenses/by/4.0/
URI : http://hdl.handle.net/10259/4873
Versión del editor: https://doi.org/10.1038/s41598-018-20708-3
Aparece en las colecciones: Artículos BIOORG

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