Manipulation of Transmembrane Transport by Synthetic K+ Ionophore Depsipeptides and Its Implications in Glucose‐Stimulated Insulin Secretion in β‐Cells.
- Resource Type
- Article
- Authors
- García‐Calvo, José; Torroba, Tomás; Brañas‐Fresnillo, Virginia; Perdomo, Germán; Cózar‐Castellano, Irene; Li, Yu‐Hao; Legrand, Yves‐Marie; Barboiu, Mihail
- Source
- Chemistry - A European Journal. Jul2019, Vol. 25 Issue 39, p9287-9294. 8p.
- Subject
- *DEPSIPEPTIDES
*PANCREATIC beta cells
*INSULIN
*SECRETION
*IONOPHORES
- Language
- ISSN
- 0947-6539
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. [ABSTRACT FROM AUTHOR]