Article
Insights into agonist-elicited activation of the human glucose-dependent insulinotropic polypeptide receptor.
Biochemical pharmacology - 1 Oct 2021
Yuliantie Elita, van der Velden Wijnand J C, Labroska Viktorija, Dai Antao, Zhao Fenghui, Darbalaei Sanaz, Deganutti Giuseppe, Xu Tongyang, Zhou Qingtong, Yang Dehua, Rosenkilde Mette M, Sexton Patrick M, Wang Ming-Wei, Wootten Denise
Abstract excerpt
Glucose-dependent insulinotropic polypeptide (GIP) and its receptor (GIPR) are part of the incretin system that regulates glucose homeostasis. A series of GIPR residues putatively important for ligand binding and receptor activation were mutated and pharmacologically evaluated using GIPR selective agonists in cAMP accumulation, ERK1/2 phosphorylation (pERK1/2) and β-arrestin 2 recruitment assays. The impact of...
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