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gastric inhibitory polypeptide receptor; GIP receptor; GIP-R; glucose-dependent insulinotropic polypeptide receptor (GIPR)
Function:
- receptor for gastric inhibitory polypeptide (GIP)
- activity is mediated by Gi proteins
- stimulates insulin release during hyperglycemia [2]
- stimulates glucagon release during hypoglycemia [2]
- suppresses food intake
Structure: belongs to the G-protein coupled receptor 2 family
Compartment: cell membrane
Alternative splicing: named isoforms=2
Expression:
- hypothalamus [3]
- arcuate nucleus, dorsomedial nucleus, paraventricular nucleus
Pharmacology:
- tirzepatide, a dual GLP-1 receptor agonist & GIP receptor agonist, is an investigational agent for treatment of diabetest mellitus type-2 [2]
General
glycoprotein
G-protein coupled receptor; serpentine receptor
Properties
SIZE: entity length = 466 aa
MW = 53 kD
COMPARTMENT: cellular membrane
MOTIF: signal sequence {1-21}
exoplasmic domain {22-138}
MOTIF: N-glycosylation site {N62}
N-glycosylation site {N77}
transmembrane domain {139-161}
cytoplasmic loop {162-169}
transmembrane domain {170-189}
exoplasmic loop {190-217}
transmembrane domain {218-242}
cytoplasmic loop {243-254}
transmembrane domain {255-278}
exoplasmic loop {279-293}
transmembrane domain {294-319}
cytoplasmic loop {320-341}
transmembrane domain {342-362}
exoplasmic loop {363-377}
transmembrane domain {378-398}
cytoplasmic domain {399-466}
Database Correlations
OMIM 137241
UniProt P48546
PFAM correlations
Kegg hsa:2696
References
- UniProt :accession P48546
- Rosenstock J, Wysham C, Frias JP, et al.
Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist
tirzepatide in patients with type 2 diabetes (SURPASS-1): A double-blind,
randomised, phase 3 trial.
Lancet 2021 Jun 25; [e-pub].
PMID: 34186022
https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(21)01324-6/fulltext
- Frias JP, Davies MJ, Rosenstock J et al.
Tirzepatide versus semaglutide once weekly in patients with type 2 diabetes.
N Engl J Med 2021 Jun 25; [e-pub].
PMID: 34170647
https://www.nejm.org/doi/10.1056/NEJMoa2107519
- Adriaenssens AE, Biggs EK, Darwish T et al
Glucose-Dependent Insulinotropic Polypeptide Receptor-Expressing Cells in the
Hypothalamus Regulate Food Intake.
Cell Metab. 2019 Nov 5;30(5):987-996.e6.
PMID: 31447324 PMCID: PMC6838660 Free PMC article.