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10 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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BDKRB1
bradykinin receptor B1
Chromosome 14 · 14q32.2
NCBI Gene: 623Ensembl: ENSG00000100739.12HGNC: HGNC:1029UniProt: P46663
114PubMed Papers
20Diseases
3Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
CLINICAL
Clinical Trials
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
protein bindingbradykinin receptor activityplasma membraneG protein-coupled receptor signaling pathwayovarian dysfunctionangioedemaresponse to angiotensin-converting enzyme inhibitorneoplasm
✦AI Summary

BDKRB1 encodes the bradykinin receptor B1, a G protein-coupled receptor with preferential affinity for kinin metabolites lacking the C-terminal arginine, such as des-Arg9-BK 1. The receptor is characterized by low basal expression but significant upregulation following tissue injury and inflammation 1. BDKRB1 is located on chromosome 14.1-q32.2 as a single-copy gene and shows widespread tissue distribution, with notable expression in kidney and pancreas 2. Mechanistically, BDKRB1 activation triggers calcium influx and activates downstream signaling pathways including MEK1-ERK1/2-NF-κB 3 and Ca2+/CaMKII/MEK1/ERK cascades 4. The receptor plays pathological roles in multiple diseases: it exacerbates sepsis by inducing neutrophil dysfunction and CXCR2 desensitization 5, promotes glioblastoma cell migration and invasion through AQP4 upregulation 3, and contributes to systemic sclerosis fibrosis through sCD13 signaling 6. BDKRB1 represents a promising therapeutic target, as antagonists improve outcomes in sepsis when combined with antibiotics 5 and show antifibrotic effects 6. The receptor is also being investigated as a target for novel analgesic development 7.

Sources cited
1
BDKRB1 has weak affinity for intact bradykinin but strong affinity for C-terminal arginine-lacking metabolites; expression is upregulated following tissue injury and inflammation
PMID: 8660997
2
BDKRB1 is a single-copy gene located on chromosome 14q32.1-q32.2 with widespread tissue distribution
PMID: 8808279
3
BDKRB1 activation triggers calcium influx and MEK1-ERK1/2-NF-κB signaling, promoting glioblastoma cell migration and invasion
PMID: 32182968
4
BDKRB1 exacerbates sepsis by inducing neutrophil dysfunction and CXCR2 desensitization; antagonists improve survival when combined with antibiotics
PMID: 41355798
5
BDKRB1 contributes to systemic sclerosis fibrosis through sCD13 signaling; targeting this axis shows antifibrotic potential
PMID: 39175116
6
BDKRB1 mediates mechanical stress-induced calcium influx and cell growth through Ca2+/CaMKII/MEK1/ERK signaling
PMID: 40296124
7
BDKRB1 is a target for new analgesic substance development
PMID: 20942817
Disease Associationsⓘ20
ovarian dysfunctionOpen Targets
0.17Weak
angioedemaOpen Targets
0.10Weak
response to angiotensin-converting enzyme inhibitorOpen Targets
0.10Suggestive
neoplasmOpen Targets
0.09Suggestive
osteoarthritisOpen Targets
0.09Suggestive
glioblastoma multiformeOpen Targets
0.09Suggestive
hypertensionOpen Targets
0.08Suggestive
experimental autoimmune encephalomyelitisOpen Targets
0.08Suggestive
arthritisOpen Targets
0.08Suggestive
PainOpen Targets
0.08Suggestive
diabetic macular edemaOpen Targets
0.08Suggestive
rheumatoid arthritisOpen Targets
0.08Suggestive
postherpetic neuralgiaOpen Targets
0.07Suggestive
gliomaOpen Targets
0.07Suggestive
systemic sclerodermaOpen Targets
0.07Suggestive
glioblastomaOpen Targets
0.07Suggestive
posterior cortical atrophyOpen Targets
0.05Suggestive
anaphylaxisOpen Targets
0.05Suggestive
age-related macular degenerationOpen Targets
0.05Suggestive
wet macular degenerationOpen Targets
0.05Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets3
BI113823Phase I
Bradykinin B1 receptor antagonist
osteoarthritis
MK0686Phase II
Bradykinin B1 receptor antagonist
postherpetic neuralgia
SAFOTIBANTPhase II
Bradykinin B1 receptor antagonist
diabetic macular edema
Related Genes
KNG1Protein interaction100%GNB1Protein interaction99%GNAQProtein interaction97%AGTProtein interaction97%GNG2Protein interaction95%EDN1Protein interaction93%
Tissue Expression6 tissues
Lung
100%
Liver
94%
Brain
82%
Ovary
53%
Bone Marrow
12%
Heart
0%
Gene Interaction Network
Click a node to explore
BDKRB1KNG1GNB1GNAQAGTGNG2EDN1
PROTEIN STRUCTURE
Preparing viewer…
PDB7EIB · 3.00 Å · EM
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
1.85LoF Tolerant
pLIⓘ
0.19Tolerant
Observed/Expected LoF0.72 [0.22–1.85]
RankingsWhere BDKRB1 stands among ~20K protein-coding genes
  • #4,142of 20,598
    Most Researched114 · top quartile
  • #16,853of 17,882
    Most Constrained (LOEUF)1.85
Genes detectedBDKRB1
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Structure and genomic organization of the human B1 receptor gene for kinins (BDKRB1).
PMID: 8660997
Genomics · 1996
1.00
2
Genomic DNA sequence, expression, and chromosomal localization of the human B1 bradykinin receptor gene BDKRB1.
PMID: 8808279
Genomics · 1996
0.90
3
BDKRB1 activation induces CXCR2 desensitization in neutrophils during severe sepsis and exacerbates disease severity.
PMID: 41355798
JCI Insight · 2025
0.80
4
The Bradykinin-BDKRB1 Axis Regulates
PMID: 32182968
Cancers (Basel) · 2020
0.70
5
In vivo DNase I-mediated footprinting analysis along the human bradykinin B1 receptor (BDKRB1) gene promoter: evidence for cell-specific regulation.
PMID: 15705059
Biochem J · 2005
0.60