Bradykinin receptor B1

Bradykinin receptor B1 (B₁) is a G-protein coupled receptor encoded by the BDKRB1 gene in humans. Its principal ligand is bradykinin, a 9 amino acid peptide generated in pathophysiologic conditions such as inflammation, trauma, burns, shock, and allergy. The B₁ receptor is one of two of G protein-coupled receptors that have been found which bind bradykinin and mediate responses to these pathophysiologic conditions.

BDKRB1
Identifiers
Aliases	BDKRB1, B1BKR, B1R, BDKRB2, BKB1R, BKR1, BRADYB1, Bradykinin receptor B1
External IDs	OMIM: 600337; MGI: 88144; HomoloGene: 570; GeneCards: BDKRB1; OMA:BDKRB1 - orthologs
Gene location (Human) Chr. Chromosome 14 (human) Band 14q32.2 Start 96,256,210 bp End 96,268,967 bp
Gene location (Mouse) Chr. Chromosome 12 (mouse) Band 12|12 E Start 105,569,344 bp End 105,571,687 bp
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in gonad testicle gallbladder stromal cell of endometrium mucosa of transverse colon ectocervix canal of the cervix vagina body of pancreas appendix Top expressed in choroid plexus of fourth ventricle entorhinal cortex embryo morula zygote secondary oocyte morula embryo primary oocyte lip More reference expression data BioGPS More reference expression data
Gene ontology Molecular function G protein-coupled receptor activity peptide binding signal transducer activity protein binding bradykinin receptor activity Cellular component integral component of membrane membrane plasma membrane integral component of plasma membrane endoplasmic reticulum neuron projection Biological process negative regulation of protein phosphorylation negative regulation of blood pressure positive regulation of leukocyte migration positive regulation of cytosolic calcium ion concentration response to stress response to mechanical stimulus positive regulation of release of sequestered calcium ion into cytosol response to lipopolysaccharide protein kinase C-activating G protein-coupled receptor signaling pathway negative regulation of cell growth sensory perception of pain inflammatory response cell migration signal transduction G protein-coupled receptor signaling pathway Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 623 12061 Ensembl ENSG00000100739 ENSMUSG00000041347 UniProt P46663 Q61125 RefSeq (mRNA) NM_000710 NM_001386007 NM_007539 RefSeq (protein) NP_000701 NP_031565 Location (UCSC) Chr 14: 96.26 – 96.27 Mb Chr 12: 105.57 – 105.57 Mb PubMed search
Wikidata
View/Edit Human View/Edit Mouse

B₁ protein is synthesized de novo following tissue injury and receptor binding leads to an increase in the cytosolic calcium ion concentration, ultimately resulting in chronic and acute inflammatory responses.

Classical agonist of this receptor includes bradykinin1-8 (bradykinin with the first 8 amino acid) and antagonist includes [Leu8]-bradykinin1-8.

Antagonists

• LF22-0542

See also

• Bradykinin receptor

External links

• "Bradykinin Receptors: B₁". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2016-03-03. Retrieved 2008-11-25.
• Human BDKRB1 genome location and BDKRB1 gene details page in the UCSC Genome Browser.
• Human BDKRB2 genome location and BDKRB2 gene details page in the UCSC Genome Browser.

Further reading

• Duchene J, Lecomte F, Ahmed S, Cayla C, Pesquero J, Bader M, Perretti M, Ahluwalia A (2007). "A novel inflammatory pathway involved in leukocyte recruitment: role for the kinin B1 receptor and the chemokine CXCL5". J. Immunol. 179 (7): 4849–56. doi:10.4049/jimmunol.179.7.4849. PMC 3696729. PMID 17878384.
• Calixto JB, Medeiros R, Fernandes ES, et al. (2005). "Kinin B1 receptors: key G-protein-coupled receptors and their role in inflammatory and painful processes". Br. J. Pharmacol. 143 (7): 803–18. doi:10.1038/sj.bjp.0706012. PMC 1575942. PMID 15520046.
• Menke JG, Borkowski JA, Bierilo KK, et al. (1994). "Expression cloning of a human B1 bradykinin receptor". J. Biol. Chem. 269 (34): 21583–6. doi:10.1016/S0021-9258(17)31844-6. PMID 8063797.
• Yang X, Polgar P (1996). "Genomic structure of the human bradykinin B1 receptor gene and preliminary characterization of its regulatory regions". Biochem. Biophys. Res. Commun. 222 (3): 718–25. doi:10.1006/bbrc.1996.0810. PMID 8651911.
• Bachvarov DR, Hess JF, Menke JG, et al. (1996). "Structure and genomic organization of the human B1 receptor gene for kinins (BDKRB1)". Genomics. 33 (3): 374–81. doi:10.1006/geno.1996.0213. PMID 8660997.
• Chai KX, Ni A, Wang D, et al. (1996). "Genomic DNA sequence, expression, and chromosomal localization of the human B1 bradykinin receptor gene BDKRB1". Genomics. 31 (1): 51–7. doi:10.1006/geno.1996.0008. PMID 8808279.
• Leeb T, Mathis SA, Leeb-Lundberg LM (1997). "The sixth transmembrane domains of the human B1 and B2 bradykinin receptors are structurally compatible and involved in discriminating between subtype-selective agonists". J. Biol. Chem. 272 (1): 311–7. doi:10.1074/jbc.272.1.311. PMID 8995263.
• Blaukat A, Herzer K, Schroeder C, et al. (1999). "Overexpression and functional characterization of kinin receptors reveal subtype-specific phosphorylation". Biochemistry. 38 (4): 1300–9. doi:10.1021/bi981727r. PMID 9930991.
• Cassano G, Susca F, Lippe C, Guanti G (1999). "Two B1 and B2 bradykinin receptor antagonists fail to inhibit the Ca2+ response elicited by bradykinin in human skin fibroblasts". Gen. Pharmacol. 32 (2): 239–44. doi:10.1016/S0306-3623(98)00275-4. PMID 10188626.
• Zhou X, Prado GN, Chai M, et al. (2000). "Posttranscriptional destabilization of the bradykinin B1 receptor messenger RNA: cloning and functional characterization of the 3'-untranslated region". Mol. Cell Biol. Res. Commun. 1 (1): 29–35. doi:10.1006/mcbr.1999.0105. PMID 10329474.
• Jones C, Phillips E, Davis C, et al. (1999). "Molecular characterisation of cloned bradykinin B1 receptors from rat and human". Eur. J. Pharmacol. 374 (3): 423–33. doi:10.1016/S0014-2999(99)00315-5. PMID 10422787.
• Sjuve R, Boels PJ, Uvelius B, Arner A (2000). "Up-regulation of bradykinin response in rat and human bladder smooth muscle". J. Urol. 164 (5): 1757–63. doi:10.1016/S0022-5347(05)67102-9. PMID 11025765.
• Sawant S, Snyman C, Bhoola K (2002). "Comparison of tissue kallikrein and kinin receptor expression in gastric ulcers and neoplasms". Int. Immunopharmacol. 1 (12): 2063–80. doi:10.1016/S1567-5769(01)00118-7. PMID 11710536.
• Ignjatovic T, Tan F, Brovkovych V, et al. (2002). "Novel mode of action of angiotensin I converting enzyme inhibitors: direct activation of bradykinin B1 receptor". J. Biol. Chem. 277 (19): 16847–52. doi:10.1074/jbc.M200355200. PMID 11880373.
• Newton R, Eddleston J, Haddad el-B, et al. (2002). "Regulation of kinin receptors in airway epithelial cells by inflammatory cytokines and dexamethasone". Eur. J. Pharmacol. 441 (3): 193–202. doi:10.1016/S0014-2999(01)01624-7. PMID 12063092.
• Kang DS, Leeb-Lundberg LM (2002). "Negative and positive regulatory epitopes in the C-terminal domains of the human B1 and B2 bradykinin receptor subtypes determine receptor coupling efficacy to G(q/11)-mediated [correction of G(9/11)-mediated] phospholipase Cbeta activity". Mol. Pharmacol. 62 (2): 281–8. doi:10.1124/mol.62.2.281. PMID 12130679. S2CID 86826886.
• Christiansen SC, Eddleston J, Woessner KM, et al. (2002). "Up-regulation of functional kinin B1 receptors in allergic airway inflammation". J. Immunol. 169 (4): 2054–60. doi:10.4049/jimmunol.169.4.2054. PMID 12165532.
• Lamb ME, Zhang C, Shea T, et al. (2003). "Human B1 and B2 bradykinin receptors and their agonists target caveolae-related lipid rafts to different degrees in HEK293 cells". Biochemistry. 41 (48): 14340–7. doi:10.1021/bi020231d. PMID 12450400.
• Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. Bibcode:2002PNAS...9916899M. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932.
• Kang DS, Ryberg K, Mörgelin M, Leeb-Lundberg LM (2004). "Spontaneous formation of a proteolytic B1 and B2 bradykinin receptor complex with enhanced signaling capacity". J. Biol. Chem. 279 (21): 22102–7. doi:10.1074/jbc.M402572200. PMID 15033977.
• Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The Status, Quality, and Expansion of the NIH Full-Length cDNA Project: The Mammalian Gene Collection (MGC)". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMC 528928. PMID 15489334.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.