Protein / target
Glucagon receptor
Protein at a glance
Biological role
Guanyl-nucleotide exchange factor
Primary biology
GPCR signalling
Strongest disease association
GCGR-related hyperglucagonemia
Therapeutic position
Established drug target
Research activity
Emerging research
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
G protein-coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis.
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G protein-coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase (PubMed:32193322, PubMed:38346960). Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system
Subcellular location
Domains and Gene Ontology detail (16)Hide
Gene Ontology
- Cmembrane
- Cplasma membrane
- Fglucagon receptor activity
- Fguanyl-nucleotide exchange factor activity
- Fpeptide hormone binding
- Padenylate cyclase-activating G protein-coupled receptor signaling pathway
- Padenylate cyclase-modulating G protein-coupled receptor signaling pathway
- Pcell surface receptor signaling pathway
- Pcellular response to glucagon stimulus
- Pcellular response to starvation
- Pgeneration of precursor metabolites and energy
- Pglucose homeostasis
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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G protein-coupled signalling
- ·G protein-coupled receptor for glucagon that plays a central role in the regulation of b…
- ·adenylate cyclase-activating G protein-coupled receptor signaling pathway
- ·adenylate cyclase-modulating G protein-coupled receptor signaling pathway
View underlying pathways (4)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Approved medicines with mapped indications
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.
3 medicines meet Open Targets' target-level approved-medicine definition; the 1 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
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.
Glucagon receptor agonist
Indicated for Diabetes Mellitus, Hypoglycemia
Glucagon receptor agonist
Glucagon receptor agonist
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
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 GCGR
Gene-level evidence surfaced through the gene GCGRthat 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.
View evidence synthesis (5)Hide
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.
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Drug development
14 compounds recorded · 3 approved · 11 in clinical development
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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 molecules — Strong
Antibodies — Strong
Protein degraders — Emerging
Other modalities — Strong
View underlying tractability evidence (10)Hide
Raw Open Targets tractability assessment buckets, by modality.
Clinical trials
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 (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
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.
- Trial status changed
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
- Product recall
Recall (Not Yet Classified): GLUCAGON
- Product recall
Recall (Class II): GLUCAGON
- New publicationGLP-1 Receptor Agonists.
- New publicationGLP-1, GIP, and Glucagon Agonists for Obesity Treatment: A Hunger Perspective.
- New publicationGlucagon resistance and metabolic-associated steatotic liver disease: a review of the evidence.
- New publicationNeuronal glucose sensing mechanisms and circuits in the control of insulin and glucagon secretion.
- New publicationIncretin and glucagon receptor polypharmacology in chronic kidney disease.
- New publicationDose-response effects on HbA<sub>1c</sub> and bodyweight reduction of survodutide, a dual glucagon/GLP-1 receptor agonist, compared with placebo and open-label semaglutide in people with type 2 diabetes: a randomised clinical trial.
- New publicationResults from three phase 1 trials of NNC9204-1177, a glucagon/GLP-1 receptor co-agonist: Effects on weight loss and safety in adults with overweight or obesity.
- Regulatory approval
Approval: Ogluo (EMA)
- Regulatory approval
Approval: Baqsimi (EMA)
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.
Research activity
Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.
Most cited
Recent
Europe PMC papers linked directly to this protein.