Glucose-dependent insulinotropic polypeptide receptor (GIPR) are G protein-coupled receptors belonging to the secretin receptor super-family, also known as class B1. GIPR comprises an N-terminal extracellular domain (ECD), a central domain consisting of seven transmembrane α-helices, and a C-terminal, cytoplasmic domain that mediates intracellular signal transduction by physical association with the G protein. GIPR increases insulin secretion in hyperglycemia and stimulates glucagon release in hypoglycemia. It also plays an important role in adipogenesis, islet β cell proliferation and insulin release, and is associated with type 2 diabetes, obesity and neurodegenerative diseases.