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Protein / target

Gastric inhibitory polypeptide receptor

Encoded byGIPRP48546Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
1
Approved medicines
Open Targets target-level
View by indication →
19
Clinical trials
Small-molecule tractable
Druggability
Structure with Ligand

Protein at a glance

Biological role

Gastric inhibitory peptide receptor

Strongest disease association

Obesity disorder

Via encoding gene GIPR · Genetic evidence · score 0.73

Therapeutic position

Established drug target

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

This is a receptor for GIP.

View complete UniProt function annotation

This is a receptor for GIP. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase

Subcellular location

Cell membrane
Domains and Gene Ontology detail (22)

Gene Ontology

  • Cmembrane
  • Cplasma membrane
  • FG protein-coupled peptide receptor activity
  • Fgastric inhibitory peptide receptor activity
  • Fglucagon family peptide binding
  • Fpeptide hormone binding
  • Ftransmembrane signaling receptor activity
  • Pactivation of adenylate cyclase activity
  • Padenylate cyclase-activating G protein-coupled receptor signaling pathway
  • Padenylate cyclase-modulating G protein-coupled receptor signaling pathway
  • Pcell surface receptor signaling pathway
  • Pdesensitization of G protein-coupled receptor signaling pathway

466 aa · 53 kDa · 3 isoforms

Biological roles

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Lipid & lipoprotein metabolismGOG protein-coupled signallingGO
View supporting evidence

Lipid & lipoprotein metabolism

  • ·response to fatty acid

G protein-coupled signalling

  • ·G protein-coupled peptide receptor activity
  • ·adenylate cyclase-activating G protein-coupled receptor signaling pathway
  • ·adenylate cyclase-modulating G protein-coupled receptor signaling pathway
  • ·desensitization of G protein-coupled receptor signaling pathway

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Approved medicines with mapped indications

1 medicine · 4 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Diabetes Mellitus1 medicine
Diabetes Mellitus, Type 21 medicine
Obesity1 medicine
Overweight1 medicine

Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

2

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

tirzepatide
Narrow target profileApprovedAgonist

Gastric inhibitory polypeptide receptor agonist

Indicated for Diabetes Mellitus, Diabetes Mellitus, Type 2, Obesity, Overweight

Direct interaction with this protein · 1 of 2 recorded protein targets — narrow recorded profile

retatrutide
Narrow target profilePhase 3Agonist

Gastric inhibitory polypeptide receptor agonist

Direct interaction with this protein · 1 of 3 recorded protein targets — narrow recorded profile

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene GIPR

Gene-level evidence surfaced through the gene GIPRthat encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Obesity disorder
0.92Well supported

Genetic evidence dominant · Open Targets 0.67

Diabetes Mellitus, Type 2
0.88Well supported

Clinical evidence dominant · Open Targets 0.68

Diabetes Mellitus
0.78Well supported

Genetic evidence dominant · Open Targets 0.45

Sleep Apnea, Obstructive
0.70Moderately supported

Genetic evidence dominant · Open Targets 0.41

Breast Neoplasms
0.70Moderately supported

Genetic evidence dominant · Open Targets 0.41

View evidence synthesis (5)
Obesity disorderWell supported
0.92
agreement 0.811.00
Genetic50%Clinical46%Literature4%

Open Targets aggregate 0.67 · 3 independent evidence families

Diabetes Mellitus, Type 2Well supported
0.88
agreement 0.770.99
Clinical55%Genetic39%Literature7%

Open Targets aggregate 0.68 · 3 independent evidence families

Diabetes MellitusWell supported
0.78
agreement 0.680.87
Genetic44%Clinical40%Animal model12%Literature3%

Open Targets aggregate 0.45 · 4 independent evidence families

Sleep Apnea, ObstructiveModerately supported
0.70
agreement 0.590.81
Genetic63%Clinical36%Literature1%

Open Targets aggregate 0.41 · 3 independent evidence families

Breast NeoplasmsModerately supported
0.70
agreement 0.590.80
Genetic78%Clinical14%Literature8%

Open Targets aggregate 0.41 · 3 independent evidence families

This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations
Diabetes Mellitus, Type 20.68
Obesity disorder0.67
Diabetes Mellitus0.45
Breast Neoplasms0.41
Obesity, Morbid0.41
Sleep Apnea, Obstructive0.41
Diabetes Mellitus, Type 10.38

Drug development

2 compounds recorded · 1 approved · 1 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 2 drugs that target this protein in Forefront's canonical graph (1 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (2)
RETATRUTIDEPhase 3
TIRZEPATIDEApproval

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesEmerging

Feasibility evidence (structure with ligand and high-quality ligand) — no clinical-stage drug of this modality recorded.

AntibodiesEmerging

Feasibility evidence (uniprot loc high conf and go cc high conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (small molecule binder) — no clinical-stage drug of this modality recorded.

Other modalitiesStrong

Approved Drug support this modality.

View underlying tractability evidence (8)
SM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confAB · UniProt SigP or TMHMMPR · Small Molecule BinderOC · Approved Drug

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

weight gainClinPGxplasma insulin levelsClinPGxplasma insulin levels and weight gainClinPGx

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

Clinical trials

19

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (15)

ClinicalTrials.gov via the drug-target graph.

What's happening now

12

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 2 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

  1. Trial status changed2026-07-16

    A Phase 1, Investigator- and Participant-Blinded Study to Evaluate the Effect of Retatrutide on α- and β- Cell Function and Insulin Sensitivity in Adult Participants With Type 2 Diabetes Mellitus

    Status changed to Active, not recruiting · ClinicalTrials.gov · via retatrutide

  2. New publication2026-02-16
    GLP-1 and the cardiovascular system.

    The Journal of clinical investigation · 2026 · 2 citations · Europe PMC · via tirzepatide

  3. New publication2026-01-14
    Glucagon-like receptor agonists and next-generation incretin-based medications: metabolic, cardiovascular, and renal benefits.

    Lancet (London, England) · 2026 · 9 citations · Europe PMC · via tirzepatide

  4. New publication2025-12-19
    The Roles of Incretin Hormones GIP and GLP-1 in Metabolic and Cardiovascular Health: A Comprehensive Review.

    International journal of molecular sciences · 2025 · 3 citations · Europe PMC · via tirzepatide

  5. New publication2025-07-01
    Neurodegeneration and Stroke After Semaglutide and Tirzepatide in Patients With Diabetes and Obesity.

    JAMA network open · 2025 · 16 citations · Europe PMC · via tirzepatide

  6. New publication2025-04-08
    Real-world evidence on the utilization, clinical and comparative effectiveness, and adverse effects of newer GLP-1RA-based weight-loss therapies.

    Diabetes, obesity & metabolism · 2025 · 57 citations · Europe PMC · via tirzepatide

  7. New publication2024-12-01
    Clinical Consequences of Delayed Gastric Emptying With GLP-1 Receptor Agonists and Tirzepatide.

    The Journal of clinical endocrinology and metabolism · 2024 · 53 citations · Europe PMC · via tirzepatide

  8. New publication2024-12-01
    GLP-1, GIP/GLP-1, and GCGR/GLP-1 receptor agonists: Novel therapeutic agents for metabolic dysfunction-associated steatohepatitis.

    World journal of gastroenterology · 2024 · 20 citations · Europe PMC · via tirzepatide

  9. New publication2024-11-26
    Why does GLP-1 agonist combined with GIP and/or GCG agonist have greater weight loss effect than GLP-1 agonist alone in obese adults without type 2 diabetes?

    Diabetes, obesity & metabolism · 2025 · 13 citations · Europe PMC · via tirzepatide

  10. New publication2024-08-01
    Clinical Outcomes of Tirzepatide or GLP-1 Receptor Agonists in Individuals With Type 2 Diabetes.

    JAMA network open · 2024 · 62 citations · Europe PMC · via tirzepatide

  11. New publication2024-06-14
    Tirzepatide modulates the regulation of adipocyte nutrient metabolism through long-acting activation of the GIP receptor.

    Cell metabolism · 2024 · 78 citations · Europe PMC · via tirzepatide

  12. Regulatory approval2022-09-15

    Approval: Mounjaro (EMA)

    ema · regulatory · ema · via tirzepatide

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.