RT info:eu-repo/semantics/article
T1 Manipulation of Transmembrane Transport by Synthetic K+ Ionophore Depsipeptides and Its Implications in Glucose‐Stimulated Insulin Secretion in β‐Cells
A1 García Calvo, José
A1 Torroba Pérez, Tomás
A1 Brañas‐Fresnillo, Virginia
A1 Perdomo Hernández, Germán M.
A1 Cózar Castellano, Irene
A1 Li, Yu‐Hao
A1 Legrand, Yves‐Marie
A1 Barboiu, Mihail
K1 Biological activity
K1 Fluorescent probes
K1 Insulin
K1 Ionophores
K1 Peptides
K1 Química orgánica
K1 Chemistry, Organic
AB 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.
PB Wiley-VCH Verlag
SN 0947-6539
YR 2019
FD 2019-05
LK http://hdl.handle.net/10259/6819
UL http://hdl.handle.net/10259/6819
LA eng
NO 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.
DS Repositorio Institucional de la Universidad de Burgos
RD 20-abr-2024