Manipulation of Transmembrane Transport by Synthetic K + Ionophore Depsipeptides and Its Implications in Glucose‐Stimulated Insulin Secretion in β‐Cells
Résumé
Cyclic depsipeptide Cereulide toxin it is a very well know potassium electrogenic ionophore particularly sensitive to pancreatic beta cells. The mechanistic details of specific activity are unknown. Here, we describe a series of synthetic substituted cereulide potassium ionophores that cause an impressive selective activation of glucose-induced insulin secretion in a constitutive manner in rat insulinoma INS1E cells. Our study demonstrates that a different electroneutral K+
transport mechanism by the anionic mutant depsipeptides when compared with classical electrogenic Cereulides can have an important impact of pharmacological value on gluco-sestimulated insulin secretion.
Domaines
Chimie
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