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Manipulation of Transmembrane Transport by Synthetic K + Ionophore Depsipeptides and Its Implications in Glucose‐Stimulated Insulin Secretion in β‐Cells
Author(s) -
GarcíaCalvo José,
Torroba Tomás,
BrañasFresnillo Virginia,
Perdomo Germán,
CózarCastellano Irene,
Li YuHao,
Legrand YvesMarie,
Barboiu Mihail
Publication year - 2019
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201901372
Subject(s) - depsipeptide , secretion , ionophore , insulin , chemistry , biochemistry , transmembrane protein , biology , receptor , endocrinology , membrane
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.