2026-05-30T14:39:03Zhttps://riubu.ubu.es/oai/requestoai:riubu.ubu.es:10259/68192022-08-27T00:05:17Zcom_10259_4354com_10259_5086com_10259_2604col_10259_4355
Manipulation of Transmembrane Transport by Synthetic K+ Ionophore Depsipeptides and Its Implications in Glucose‐Stimulated Insulin Secretion in β‐Cells
García Calvo, José
Torroba Pérez, Tomás
Brañas‐Fresnillo, Virginia
Perdomo Hernández, Germán M.
Cózar Castellano, Irene
Li, Yu‐Hao
Legrand, Yves‐Marie
Barboiu, Mihail
Biological activity
Fluorescent probes
Insulin
Ionophores
Peptides
Química orgánica
Chemistry, Organic
The cyclic depsipeptide cereulide toxin it is a very well-known potassium electrogenic ionophore particularly sensitive to pancreatic beta cells. The mechanistic details of its specific activity are unknown. Here, we describe a series of synthetic substituted cereulide potassium ionophores that cause impressive selective activation of glucose-induced insulin secretion in a constitutive manner in rat insulinoma INS1E cells. Our study demonstrates that the different electroneutral K+ transport mechanism exhibited by the anionic mutant depsipeptides when compared with classical electrogenic cereulides can have an important impact of pharmacological value on glucose-stimulated insulin secretion.
Ministerio de Economía y Competitividad, Spain (Projects CTQ2015-71353-R, SAF2016-77871-C2-1-R and SAF2016-77871-C2-2-R), the Junta de Castilla y León, Consejería de Educación y Cultura y Fondo Social Europeo (Project BU263P18) and the EFSD European Research Programme on New Targets for Type 2 Diabetes supported by an educational research grant from Merck Sharp & Dohme to I.C.C. and G.P. (EFSD-2017). This work was also supported in part by the 1000 Talent Plan (WQ20144400255) of State Administration of Foreign Experts Affairs, China. Y.-H.L. wishes to thank the Innovation and Talent Introduction Base of Photoelectronic and Functional Molecular Solid Material (Grant No. 90002-18011002) from Sun Yat-sen University and the China Scholarship Council (No. 21606380054) for financial support.
2022-08-26T11:50:20Z
2022-08-26T11:50:20Z
2019-05
info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
0947-6539
http://hdl.handle.net/10259/6819
10.1002/chem.201901372
1521-3765
eng
Chemistry - A European Journal. 2019, V. 25, n. 39, p. 9287-9294
https://doi.org/10.1002/chem.201901372
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/CTQ2015-71353-R/ES/DESARROLLO DE NUEVOS DISPOSITIVOS MOLECULARES FLUOROGENICOS PARA LA DETECCION RAPIDA DE AGENTES DE ORIGEN QUIMICO O BIOLOGICO DE ALTO RIESGO
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/SAF2016-77871-C2-1-R/ES/PAPEL DE INSULIN DEGRADING ENZYME (IDE) EN LA HIPERGLUCAGONEMIA
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/SAF2016-77871-C2-2-R/ES/PAPEL DE INSULIN DEGRADING ENZYME (IDE) EN LA HIPERGLUCAGONEMIA
info:eu-repo/grantAgreement/Junta de Castilla y León//BU263P18
info:eu-repo/grantAgreement/MSD/EFSD European Research Programme on New Targets for Type 2 Diabetes/EFSD-2017
info:eu-repo/grantAgreement/State Administration of Foreign Experts Affairs, China/1000 Talent Plan/WQ20144400255
info:eu-repo/grantAgreement/SYSU/Innovation and Talent Introduction Base of Photoelectronic and Functional Molecular Solid Material/90002-18011002
info:eu-repo/grantAgreement/CSC//21606380054
info:eu-repo/semantics/openAccess
application/pdf
Wiley-VCH Verlag
https://riubu.ubu.es/bitstream/10259/6819/3/Garcia-cej_2019.pdf.jpg
Hispana
TEXT
http://rightsstatements.org/vocab/CNE/1.0/
RIUBU. Repositorio Institucional de la Universidad de Burgos
http://hdl.handle.net/10259/6819