2026-04-28T08:53:51Zhttps://riubu.ubu.es/oai/requestoai:riubu.ubu.es:10259/48742021-11-10T09:38:19Zcom_10259_3924com_10259_5086com_10259_2604col_10259_3925
Cossu, Claudia
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500
Fiore, Michele
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Baroni, Debora
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500
Capurro, Valeria
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500
Caci, Emanuela
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500
García Valverde, María
222
500
Quesada Pato, Roberto
458
500
Moran, Óscar
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2018-08-21T11:45:00Z
2018-08-21T11:45:00Z
2018-08
1663-9812
http://hdl.handle.net/10259/4874
10.3389/fphar.2018.00852
Cystic fibrosis (CF) is a genetic lethal disease, originated from the defective function
of the CFTR protein, a chloride and bicarbonate permeable transmembrane channel.
CF mutations affect CFTR protein through a variety of molecular mechanisms which
result in different functional defects. Current therapeutic approaches are targeted to
specific groups of patients that share a common functional defect. We seek to develop
an innovative therapeutic approach for the treatment of CF using anionophores, small
molecules that facilitate the transmembrane transport of anions. We have characterized
the anion transport mechanism of a synthetic molecule based on the structure of
prodigiosine, a red pigment produced by bacteria. Anionophore-driven chloride efflux
from large unilamellar vesicles is consistent with activity of an uniporter carrier that
facilitates the transport of anions through lipid membranes down the electrochemical
gradient. There are no evidences of transport coupling with protons. The selectivity
sequence of the prodigiosin inspired EH160 ionophore is formate > acetate > nitrate
> chloride > bicarbonate. Sulfate, phosphate, aspartate, isothionate, and gluconate are
not significantly transported by these anionophores. Protonation at acidic pH is important
for the transport capacity of the anionophore. This prodigiosin derived ionophore induces
anion transport in living cells. Its low toxicity and capacity to transport chloride and
bicarbonate, when applied at low concentration, constitute a promising starting point
for the development of drug candidates for CF therapy.
European Union’s
Horizon 2020 research and innovation programme under grant
agreement No 667079 and Consejería de Educación de la Junta
de Castilla y León (Project BU092U16).
application/pdf
eng
Frontiers Media
Frontiers in Pharmacology. 2018, V. 9, art. 852
https://doi.org/10.3389/fphar.2018.00852
info:eu-repo/grantAgreement/EC/H2020/667079
info:eu-repo/grantAgreement/JCyL/BU092U16
Attribution 4.0 International
http://creativecommons.org/licenses/by/4.0/
info:eu-repo/semantics/openAccess
cystic fibrosis
ionophore
ion transport
phospholipid vesicles
prodigiosin derivatives
Química orgánica
Chemistry, Organic
Anion-transport mechanism of a triazole-bearing derivative of prodigiosine: a candidate for cystic fibrosis therapy
info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
CC-LICENSE
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Cossu-FP_2018.pdf.jpg
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Cossu-FP_2018.pdf
Cossu-FP_2018.pdf
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license.txt
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TEXT
Cossu-FP_2018.pdf.txt
Cossu-FP_2018.pdf.txt
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10259/4874
oai:riubu.ubu.es:10259/4874
2021-11-10 10:38:19.526
Repositorio Institucional de la Universidad de Burgos
bubrep@ubu.es
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