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10 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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ADGRD1
adhesion G protein-coupled receptor D1
Chromosome 12 · 12q24.33
NCBI Gene: 283383Ensembl: ENSG00000111452.14HGNC: HGNC:19893UniProt: Q6QNK2
35PubMed Papers
20Diseases
0Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
G protein-coupled receptor activityregulation of skeletal muscle contractionprotein bindingplasma membraneAbnormality of the skeletal systemdiaphragmatic herniaHernia of the abdominal wallsporadic amyotrophic lateral sclerosis
✦AI Summary

ADGRD1 (adhesion G protein-coupled receptor D1), also known as GPR133, is an adhesion GPCR that functions as a receptor for the potent androgen 5alpha-dihydrotestosterone (5alpha-DHT) and the drug methenolone 1. Ligand binding triggers conformational changes activating Gs-coupled G proteins, leading to adenylate cyclase activation and increased intracellular cAMP levels 21. In muscle cells, ADGRD1 enhances muscle strength through cAMP signaling 1. Beyond androgen signaling, ADGRD1 regulates bone homeostasis through dual mechanisms: it inhibits osteoclastogenesis via the cAMP-PKA-NFATC1 pathway 3, while simultaneously promoting osteoblast differentiation and bone formation through cAMP-dependent β-catenin signaling and mechanotransduction involving interaction with PTK7 4. Intracellularly, ESYT1 negatively modulates GPR133 signaling in a calcium-dependent manner 5. ADGRD1 supports glioblastoma growth 6 and shows reduced expression in non-small-cell lung cancer correlating with better prognosis 7. Recent evidence suggests ADGRD1 involvement in SARS-CoV-2 infection 8. These findings position ADGRD1 as a promising therapeutic target for osteoporosis and potentially other diseases.

Sources cited
1
ADGRD1 is an aGPCR for 5alpha-DHT and methenolone; activates Gs-coupled adenylate cyclase signaling; increases muscle strength via cAMP
PMID: 39884271
2
ADGRD1 is coupled to Gs G proteins and mediates adenylate cyclase activation
PMID: 22025619
3
ADGRD1 activation inhibits osteoclastogenesis via cAMP-PKA-NFATC1 pathway; GL64 is a selective ADGRD1 agonist; prevents bone loss in ovariectomy model
PMID: 40644539
4
ADGRD1 knockouts show osteoporotic phenotype; enhances osteoblast differentiation via cAMP-β-catenin signaling; mechanosensitive; AP503 activates ADGRD1 to alleviate osteoporosis
PMID: 40583059
5
ESYT1 is an intracellular interactor of ADGRD1 that suppresses GPR133 signaling in calcium-dependent manner
PMID: 38758649
6
PTK7 acts as a positive allosteric modulator of GPR133 signaling; GPR133 supports glioblastoma growth
PMID: 37354459
7
ADGRD1 expression is decreased in NSCLC; correlates with prognosis, TMB, and immune infiltration
PMID: 36457341
8
ADGRD1 mRNA is upregulated in SARS-CoV-2-infected lung cells; involved in viral replication and infectivity
PMID: 38786015
Disease Associationsⓘ20
Abnormality of the skeletal systemOpen Targets
0.52Moderate
diaphragmatic herniaOpen Targets
0.31Weak
Hernia of the abdominal wallOpen Targets
0.31Weak
sporadic amyotrophic lateral sclerosisOpen Targets
0.29Weak
tooth diseaseOpen Targets
0.25Weak
Hodgkins lymphomaOpen Targets
0.20Weak
spondylolisthesisOpen Targets
0.15Weak
Genu valgumOpen Targets
0.14Weak
Genu varumOpen Targets
0.14Weak
glioblastoma multiformeOpen Targets
0.10Weak
neoplasmOpen Targets
0.09Suggestive
lung adenocarcinomaOpen Targets
0.09Suggestive
gliomaOpen Targets
0.08Suggestive
non-small cell lung carcinomaOpen Targets
0.08Suggestive
heart failureOpen Targets
0.07Suggestive
crush injuryOpen Targets
0.06Suggestive
protozoa infectious diseaseOpen Targets
0.06Suggestive
crystal arthropathyOpen Targets
0.06Suggestive
neutropeniaOpen Targets
0.06Suggestive
ovarian neoplasmOpen Targets
0.05Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Related Genes
GNB1Protein interaction100%RCC1Protein interaction91%CSE1LProtein interaction84%KPNB1Protein interaction84%XPO1Protein interaction84%XPOTProtein interaction84%
Tissue Expression6 tissues
Heart
100%
Lung
86%
Ovary
47%
Liver
20%
Brain
4%
Bone Marrow
2%
Gene Interaction Network
Click a node to explore
ADGRD1GNB1RCC1CSE1LKPNB1XPO1XPOT
PROTEIN STRUCTURE
Preparing viewer…
PDB8X9T · 2.75 Å · EM
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.83LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.66 [0.53–0.83]
RankingsWhere ADGRD1 stands among ~20K protein-coding genes
  • #10,906of 20,598
    Most Researched35
  • #7,030of 17,882
    Most Constrained (LOEUF)0.83
Genes detectedADGRD1
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
International Union of Basic and Clinical Pharmacology. XCIV. Adhesion G protein-coupled receptors.
PMID: 25713288
Pharmacol Rev · 2015
1.00
2
Exogenous activation of the adhesion GPCR ADGRD1/GPR133 protects against bone loss by negatively regulating osteoclastogenesis.
PMID: 40644539
Sci Adv · 2025
0.90
3
The mechanosensitive adhesion G protein-coupled receptor 133 (GPR133/ADGRD1) enhances bone formation.
PMID: 40583059
Signal Transduct Target Ther · 2025
0.80
4
Modulation of GPR133 (ADGRD1) signaling by its intracellular interaction partner extended synaptotagmin 1.
PMID: 38758649
Cell Rep · 2024
0.70
5
PTK7 is a positive allosteric modulator of GPR133 signaling in glioblastoma.
PMID: 37354459
Cell Rep · 2023
0.60