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Bioconjug Chem. 2014 Jan 15;25(1):171-7. doi: 10.1021/bc4005014. Epub 2013 Dec 20.

Fluorescent exendin-4 derivatives for pancreatic β-cell analysis.

Author information

1
Center for Systems Biology, Massachusetts General Hospital , 185 Cambridge Street, CPZN 5206, Boston, Massachusetts 02114, United States.

Abstract

The ability to reliably identify pancreatic β-cells would have far reaching implications for a greater understanding of β-cell biology, measurement of β-cell mass in diabetes, islet transplantation, and drug development. The glucagon-like peptide-1 receptor (GLP1R) is highly expressed on the surface of insulin producing pancreatic β-cells. Using systematic modifications of the GLP1R ligand, exendin-4, we screened over 25 compounds and identified a palette of fluorescent exendin-4 with high GLP1R binding affinity. We show considerable differences in affinity, as well as utility of the top candidates for flow cytometry and microscopy of β-cells. Some of the developed compounds should be particularly useful for basic and translational β-cell research.

PMID:
24328216
PMCID:
PMC4016126
DOI:
10.1021/bc4005014
[Indexed for MEDLINE]
Free PMC Article

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