2026-05-12T09:24:04Zhttps://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 198 600 Torroba Pérez, Tomás 554 600 Brañas‐Fresnillo, Virginia 3c2011dd-5dac-470f-9f8b-a2df5783ddac Perdomo Hernández, Germán M. 433 600 Cózar Castellano, Irene 3f72cbc3-d322-4e0a-a780-4e0fc4965813 600 Li, Yu‐Hao 96789fad-0e47-4bfb-8d58-a0f1a7ec0b4f Legrand, Yves‐Marie f5082fbc-4bcb-4ddd-be2e-7a8a25d22596 Barboiu, Mihail c839ea63-f1d5-435c-9186-7e06bbe4ee2b 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 THUMBNAIL Garcia-cej_2019.pdf.jpg Garcia-cej_2019.pdf.jpg IM Thumbnail image/jpeg 3759 https://riubu.ubu.es/bitstream/10259/6819/3/Garcia-cej_2019.pdf.jpg 431ebbcf5aa7bb517f69cd3cf5c4eff2 MD5 3 LICENSE license.txt license.txt text/plain; charset=utf-8 999 https://riubu.ubu.es/bitstream/10259/6819/2/license.txt b295bcbce42e2caabeb0c623d3860c06 MD5 2 ORIGINAL Garcia-cej_2019.pdf Garcia-cej_2019.pdf application/pdf 1696496 https://riubu.ubu.es/bitstream/10259/6819/1/Garcia-cej_2019.pdf ae82d446c8ac3de9331e9302d0cada61 MD5 1 10259/6819 oai:riubu.ubu.es:10259/6819 2022-08-27 02:05:17.718 Repositorio Institucional de la Universidad de Burgos bubrep@ubu.es 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