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Org Lett. 2013 Oct 18;15(20):5318-21. doi: 10.1021/ol402568j. Epub 2013 Oct 2.

A β-peptide agonist of the GLP-1 receptor, a class B GPCR.

Author information

1
Department of Chemistry, Yale University , New Haven, Connecticut 06511, United States, Department of Internal Medicine, Yale University School of Medicine , New Haven, Connecticut 06536, United States, Department of Cell Biology, Yale University School of Medicine , New Haven, Connecticut 06520, United States, Department of Cellular and Molecular Physiology, Yale University School of Medicine , New Haven, Connecticut 06520, United States, Howard Hughes Medical Institute, Yale University School of Medicine , New Haven, Connecticut 06520, United States, and Department of Molecular, Cellular and Developmental Biology, Yale University , New Haven, Connecticut 06520, United States.

Abstract

Previous work has shown that certain β(3)-peptides can effectively mimic the side chain display of an α-helix and inhibit interactions between proteins, both in vitro and in cultured cells. Here we describe a β(3)-peptide analog of GLP-1, CC-3(Act), that interacts with the GLP-1R extracellular domain (nGLP-1R) in vitro in a manner that competes with exendin-4 and induces GLP-1R-dependent cAMP signaling in cultured CHO-K1 cells expressing GLP-1R.

PMID:
24087900
PMCID:
PMC4006878
DOI:
10.1021/ol402568j
[Indexed for MEDLINE]
Free PMC Article

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