2026-10-29T14:55:11Zhttps://riubu.ubu.es/oai/request

oai:riubu.ubu.es:10259/48732024-01-13T19:49:40Zcom_10259_3924com_10259_5086com_10259_2604col_10259_3925

Hernando Santa Cruz, Elsa Capurro, Valeria Cossu, Claudia Fiore, Michele García Valverde, María Soto Cerrato, Vanessa Pérez Tomás, Ricardo Moran, Óscar Zegarra Moran, Olga Quesada Pato, Roberto 2018-02 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. application/pdf http://hdl.handle.net/10259/4873 eng Nature Research Small molecule anionophores promote transmembrane anion permeation matching CFTR activity info:eu-repo/semantics/article TEXT RIUBU. Repositorio Institucional de la Universidad de Burgos Hispana