2026-06-29T22:15:44Zhttps://riubu.ubu.es/oai/request

oai:riubu.ubu.es:10259/68192022-08-27T00:05:17Zcom_10259_4354com_10259_5086com_10259_2604col_10259_4355

García Calvo, José Torroba Pérez, Tomás Brañas‐Fresnillo, Virginia Perdomo Hernández, Germán M. Cózar Castellano, Irene Li, Yu‐Hao Legrand, Yves‐Marie Barboiu, Mihail 2022-08-26T11:50:20Z 2022-08-26T11:50:20Z 2019-05 0947-6539 http://hdl.handle.net/10259/6819 10.1002/chem.201901372 1521-3765 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. application/pdf eng Wiley-VCH Verlag 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 Biological activity Fluorescent probes Insulin Ionophores Peptides Química orgánica Chemistry, Organic Manipulation of Transmembrane Transport by Synthetic K+ Ionophore Depsipeptides and Its Implications in Glucose‐Stimulated Insulin Secretion in β‐Cells info:eu-repo/semantics/article info:eu-repo/semantics/acceptedVersion info:eu-repo/semantics/openAccess Chemistry – A European Journal 25 39 9287 9294