Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 25, Issue 39, Pages 9287-9294Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201901372
Keywords
biological activity; fluorescent probes; insulin; ionophores; peptides
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Funding
- China Scholarship Council [21606380054] Funding Source: Medline
- Ministerio de Economía, Industria y Competitividad, Gobierno de España [CTQ2015-71353-R] Funding Source: Medline
- SAFEA State Administration of Foregn Experts Affairs, China [1000 Talent Plan WQ20144400255] Funding Source: Medline
- Sun Yat-sen University [Talent Introduction Base of Photoelectronic and Functional Molecular Solid Material (Grant No. 90002-18011002)] Funding Source: Medline
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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.
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