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Insights into agonist-elicited activation of the human glucose-dependent insulinotropic polypeptide receptor

Biochem Pharmacol. 2021-07; 
Elita Yuliantie, Wijnand J C van der Velden, Viktorija Labroska, Antao Dai, Fenghui Zhao, Sanaz Darbalaei, Giuseppe Deganutti, Tongyang Xu, Qingtong Zhou, Dehua Yang, Mette M Rosenkilde, Patrick M Sexton, Ming-Wei Wang, Denise Wootten
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Mutant Libraries … The pcDNA3.1(+) plasmids encoding the native human or mutant GIPRs were purchased from GenScript (Piscataway, NJ, USA). The next day, cells were transfected with 0.33 µg WT or mutant GIPR, 0.042 µg Rluc8-Arrestin3-SP1 (arrestin3 = β-arrestin 2), 0.8 µg mem-citrine-… Get A Quote

摘要

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 mutation on ligand efficacy was determined by operational modelling of experimental data for each mutant, with results mapped onto the full-length, active-state GIPR structure. Two interaction networks, comprising transmembrane helix (TM) 7, TM1 and TM2, and extracellular loop (ECL) 2, TM5 and ECL3 were ... More

关键词

Arrestin, ERK, G protein-coupled receptor, GPCR structure–function relationship, Glucose-dependent insulinotropic polypeptide receptor, cAMP