ArticleStable expression of the rat GLP-I receptor in CHO cells: Activation and binding characteristics utilizing GLP-I(7–36)-amide, oxyntomodulin, exendin-4, and exendin(9–39)
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Chronic hyperglycemia downregulates GLP-1 receptor signaling in pancreatic β-cells via protein kinase A
2015, Molecular MetabolismCitation Excerpt :This indicates that other stimuli of the cAMP/PKA signaling system are also likely to lead to loss of the GLP-1R from the cell surface. Since GLP-1R activation itself raises cAMP and activates PKA [2,40], chronic exposure to GLP-1R agonists should also reduce cell surface GLP-1R and impair downstream signaling. Consistent with this hypothesis, chronic exposure of MIN6 cells cultured at low glucose in the presence of the GLP-1R agonist exendin-4, led to the dramatic loss of fluorescein-tagged exendin-4 binding to the cell surface (Figure 7A).
Oxyntomodulin attenuates exendin-4-induced hypoglycemia in cattle
2013, Domestic Animal EndocrinologyCitation Excerpt :In support of that previous report, this study showed that the insulin-releasing effects of OXM and glucagon were suppressed in the presence of GLP-1 and Ex-4. Regarding the binding to and activation of GLP-1R by GLP-1, Ex-4, and OXM, Fehmann et al [32] reported that the potential to displace 125I-GLP-1 from GLP-1R was GLP-1 > Ex-4 > OXM and to stimulate cyclic adenosine monophosphate production was GLP-1 = Ex-4 > OXM. To our best knowledge, no report of a comparison of binding and activation of Ex-4 and glucagon to GLP-1R is available.
Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function
2012, Journal of Biological ChemistryCitation Excerpt :In this study, we have used alanine scanning of residues of ECL2 and adjacent amino acids to examine the role of these residues in binding and signaling mediated by peptide and nonpeptide ligands of the GLP-1R, a family B GPCR. Exendin-4 is a high affinity GLP-1 peptide mimetic currently approved for clinical treatment of type II diabetics (3, 27, 28), although oxyntomodulin is a naturally occurring GLP-1R peptide ligand with intermediate potency between full-length and truncated GLP-1 peptides (1, 29). In accord with observations for GLP-1 peptides in our accompanying article (18), ECL2 was critically important for activation transition of the GLP-1R by exendin-4 and oxyntomodulin, albeit with distinctions in the involvement of individual residues.
Synthesis and evaluation of [ <sup>18</sup>F]exendin (9-39) as a potential biomarker to measure pancreatic β-cell mass
2012, Nuclear Medicine and BiologyApplication of novel peptide (Pp1) improving the half-life of exendin-4 in vivo
2011, PeptidesCitation Excerpt :Although a mammalian homolog does not seem to exist [18], exendin-4 shares 53% identity at the amino acid level with the mammalian hormone glucagon-like peptide-1 (GLP-1) [5]. Exendin-4 is a natural analog of GLP-1 that binds and activates the GLP-1 receptor in the same manner as GLP-1 [8,11,20]. GLP-1 is a peptide produced from the endocrine L-cells of the gut in response to oral glucose administration, and it functions as an incretin hormone [11].
Gut hormones: Implications for the treatment of obesity
2009, Pharmacology and Therapeutics