Literature DB >> 24087900

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

Elizabeth V Denton1, Cody J Craig, Rebecca L Pongratz, Jacob S Appelbaum, Amy E Doerner, Arjun Narayanan, Gerald I Shulman, Gary W Cline, Alanna Schepartz.   

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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Year:  2013        PMID： 24087900      PMCID： PMC4006878          DOI： 10.1021/ol402568j

Source DB:  PubMed          Journal:  Org Lett        ISSN： 1523-7052            Impact factor:   6.005


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