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Updated: May 7, 2026

Mechanisms Underlying Gut Hormone Secretion Using the Isolated Perfused Rat Small Intestine
Published on: February 26, 2019
A β-peptide agonist of the GLP-1 receptor, a class B GPCR
Elizabeth V Denton1, Cody J Craig, Rebecca L Pongratz
1Department 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.
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