GIPR notes

Deep research

• just deep-research-falcon human GIPR --fallback perplexity-lite failed (providers unavailable,
  2026-10-21). Notes from cached publications and UniProt P48546.

Function

• Class B1 GPCR for glucose-dependent insulinotropic polypeptide (GIP). Human islet receptor clones showed
  high-affinity GIP binding; "GIP binding to both forms of the receptor induced a dose-dependent increase in
  intracellular cAMP levels (EC50 values of 0.6-0.8 nmol/l) but no elevation of cytoplasmic calcium
  concentrations" PMID:7556958. Insulinoma clone coupled to adenylate cyclase and did not raise Ca2+
  PMID:7589426.
• GIP binds in a surface groove of the ECD PMID:17715056; truncated GIP(3-30)NH2 is a competitive
  antagonist at human GIPR in COS-7 cAMP assays PMID:26572091.
• GWAS: GIPR variants associated with 2-h glucose, reduced insulin secretion and diminished incretin effect
  PMID:20081857.
• RAMP complexes from multiplexed screen PMID:39083597.

Localization

• Seven-TM receptor, ECD aa 22-138 extracellular. "N-glycosylation is required for cell surface expression"
  (UniProt, PMID:22412906). Conclusion: plasma membrane, ligand-binding ECD exposed.