The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)



Gene Review

BDKRB1  -  bradykinin receptor B1

Homo sapiens

Synonyms: B1 bradykinin receptor, B1BKR, B1R, BDKRB2, BK-1 receptor, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of BDKRB1


High impact information on BDKRB1

  • Because a better understanding of the mechanism of the upregulation will help in understanding its potential importance in inflammation, we have studied the molecular mechanism of B1-receptor upregulation in cultured human lung fibroblasts (IMR 90) in response to IL-1beta and the B1-agonist [des-Arg10]-kallidin [6].
  • BK-induced IL-1beta synthesis was inhibited by a B2-type BK receptor antagonist and by treatment of the cells with pertussis toxin, indicating the involvement of a BK receptor that couples to the G(i)/G(o) class of heterotrimeric G proteins [7].
  • Allelic polymorphisms affecting exon 3 of the B1 receptor gene (A1098-->G) or exon 2 (C181-->T) or 1 (a 9-base pair deletion) of the B2 receptor gene were found to be neutral [8].
  • Altered frequency of a promoter polymorphic allele of the kinin B1 receptor gene in inflammatory bowel disease [8].
  • RESULTS: Only the B1 receptor promoter polymorphism (G-699-->C) exhibited a significantly different allele frequency between the two groups (prevalence of the C allele of 5.7% in patients with IBD compared with 33.6% in controls; P = 0.0002) or between the controls and either etiologic subgroup (ulcerative colitis and Crohn's disease) [8].

Chemical compound and disease context of BDKRB1

  • OBJECTIVE: To identify variants in the complete genomic sequence of the two subtypes of bradykinin receptors: B1 (BDKRB1) and B2 (BDKRB2) and to examine the association of these variants with essential hypertension [1].
  • Using androgen-insensitive prostate cancer PC3 cells, we show that specific stimulation of endogenous B1R promotes cell growth, migration, and invasion [9].
  • The present results support that compound 11 is a potent and highly selective antagonist suitable for further investigations of the role of the kinin B1R in models of inflammation, pain, and sepsis based on the rabbit [10].
  • We investigated the expression and localization of B1 receptor in tissues of rats submitted to a renin-dependent model of hypertension (2K-1C), and analyzed the influence of endogenous Ang II in modulating the in vivo expression of these receptors [11].
  • Diabetic hyperalgesia is absent in streptozotocin-induced type 1 diabetic BKB1-R knockout mice [12].

Biological context of BDKRB1


Anatomical context of BDKRB1

  • In the present study we used the highly sensitive DNase I in vivo footprinting approach to delineate more precisely the functional domains of the BDKRB1 gene promoter in human SMCs (smooth muscle cells) [14].
  • The photoprotein aequorin was utilized as an indicator of the ability of the B1 receptor agonist [des-Arg10]kallidin to mediate Ca2+ mobilization in Xenopus laevis oocytes injected with RNA [15].
  • Here, we show that B1R spontaneously forms a proteolytic plasma membrane complex with B2R along with increased receptor signaling capacity [16].
  • Northern blot analysis identified a 1.7- to 1.8-kb mature mRNA transcript of the B1 receptor gene in the kidney and pancreas [13].
  • Bradykinin (BK)-related peptides are suspected to negatively influence diverse functions in vascular smooth muscle cells (SMCs), notably via stimulation of the inducible B1 receptor (B1R), and have been shown to inhibit the migration of rat SMCs [17].

Associations of BDKRB1 with chemical compounds

  • Human lymphocytes that do not express a functional BDKRB1 were also studied as a reference using dimethyl sulphate, UV light type C and DNase I treatments [14].
  • The cloned B1 bradykinin receptor expressed in mammalian cells exhibits high affinity binding for 3H-labeled [des-Arg10]kallidin and low affinity for bradykinin [15].
  • Constitutive B1R activity was further increased by alanine mutation of Asn(121) in the third transmembrane domain of the receptor (B1A(121)) [18].
  • Studies with BK receptor antagonists and agonists indicate that inositol lipid signalling and arachidonic acid mobilization in response to BK are B2 receptor-mediated pathways, whereas the inhibition of DNA synthesis appears to be via B1 receptors [19].
  • High-affinity binding of peptide agonists to the human B1 bradykinin receptor depends on interaction between the peptide N-terminal L-lysine and the fourth extracellular domain of the receptor [20].

Physical interactions of BDKRB1

  • These findings indicate, for the first time, that the BK receptor is coupled to the important protooncogene c-src and that the src pathway may mediate some of the events downstream from BK binding [21].

Regulatory relationships of BDKRB1


Other interactions of BDKRB1

  • Selective immunoprecipitation with epitope-specific antibodies revealed a spontaneously formed heterologous receptor complex, which was composed of the intact 35-kDa B1R and the B2R degradation products [16].
  • We investigated whether cyclooxygenase (COX)-2 induction was involved in prostaglandin (PG) E2 release by BK in cultured human airway smooth muscle (ASM) cells and analyzed the BK receptor subtypes responsible [27].
  • Although these data support a role for prostaglandins and EGF receptor down-modulation in the inhibitory action of BK on DNA synthesis in breast fibroblasts, a B1 receptor-mediated pathway is also implicated [19].
  • We investigated the contribution of the B1 receptor to the maintenance of vascular tone and t-PA release in patients with heart failure [28].
  • We examined B1 receptor mRNA expression in nasal tissue samples from allergic rhinitis and normal subjects [29].

Analytical, diagnostic and therapeutic context of BDKRB1

  • No significant changes in the promoter foot-printing pattern were found after treatment with interleukin-1beta or serum (known BDKRB1 gene inducers), indicating that definite regulatory motifs could exist outside the BDKRB1 gene core promoter region studied [14].
  • Genomic Southern blot analysis indicated that the human B1 receptor is encoded by a single-copy gene [3].
  • Previous works have shown a neuroprotector effect for kinin B2 receptor and a deleterious, pro-epileptogenic action for kinin B1 receptor in animal models of TLE [30].
  • CLR contained B2R and B1R as determined by both receptor immunoblotting and the increase in specific activity of receptor agonist binding to cells at both 4 and 37 degrees C when binding was followed by CLR enrichment [31].
  • The new compounds were tested against the contractile effect induced by desArg9BK on 2 B1 receptor bioassays, the human umbilical vein, and the rabbit aorta [32].


  1. Sequence variation of bradykinin receptors B1 and B2 and association with hypertension. Cui, J., Melista, E., Chazaro, I., Zhang, Y., Zhou, X., Manolis, A.J., Baldwin, C.T., Destefano, A.L., Gavras, H. J. Hypertens. (2005) [Pubmed]
  2. Characterization of two polymorphic sites in the human kinin B1 receptor gene: altered frequency of an allele in patients with a history of end-stage renal failure. Bachvarov, D.R., Landry, M., Pelletier, I., Chevrette, M., Betard, C., Houde, I., Bergeron, J., Lebel, M., Marceau, F. J. Am. Soc. Nephrol. (1998) [Pubmed]
  3. Structure and genomic organization of the human B1 receptor gene for kinins (BDKRB1). Bachvarov, D.R., Hess, J.F., Menke, J.G., Larrivée, J.F., Marceau, F. Genomics (1996) [Pubmed]
  4. Kinin B1 receptor expression on multiple sclerosis mononuclear cells: correlation with magnetic resonance imaging T2-weighted lesion volume and clinical disability. Prat, A., Biernacki, K., Saroli, T., Orav, J.E., Guttmann, C.R., Weiner, H.L., Khoury, S.J., Antel, J.P. Arch. Neurol. (2005) [Pubmed]
  5. Immunolocalization and expression of kinin B1R and B2R receptors in human inflammatory bowel disease. Stadnicki, A., Pastucha, E., Nowaczyk, G., Mazurek, U., Plewka, D., Machnik, G., Wilczok, T., Colman, R.W. Am. J. Physiol. Gastrointest. Liver Physiol. (2005) [Pubmed]
  6. The B1-agonist [des-Arg10]-kallidin activates transcription factor NF-kappaB and induces homologous upregulation of the bradykinin B1-receptor in cultured human lung fibroblasts. Schanstra, J.P., Bataillé, E., Marin Castaño, M.E., Barascud, Y., Hirtz, C., Pesquero, J.B., Pecher, C., Gauthier, F., Girolami, J.P., Bascands, J.L. J. Clin. Invest. (1998) [Pubmed]
  7. Bradykinin stimulates NF-kappaB activation and interleukin 1beta gene expression in cultured human fibroblasts. Pan, Z.K., Zuraw, B.L., Lung, C.C., Prossnitz, E.R., Browning, D.D., Ye, R.D. J. Clin. Invest. (1996) [Pubmed]
  8. Altered frequency of a promoter polymorphic allele of the kinin B1 receptor gene in inflammatory bowel disease. Bachvarov, D.R., Landry, M., Houle, S., Paré, P., Marceau, F. Gastroenterology (1998) [Pubmed]
  9. Bradykinin receptor subtype 1 expression and function in prostate cancer. Taub, J.S., Guo, R., Leeb-Lundberg, L.M., Madden, J.F., Daaka, Y. Cancer Res. (2003) [Pubmed]
  10. A novel nonpeptide antagonist of the kinin B1 receptor: effects at the rabbit receptor. Morissette, G., Fortin, J.P., Otis, S., Bouthillier, J., Marceau, F. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  11. Modulation of kinin B1 receptor expression by endogenous angiotensin II in hypertensive rats. Fernandes, L., Ceravolo, G.S., Fortes, Z.B., Tostes, R., Santos, R.A., Santos, J.A., Mori, M.A., Pesquero, J.B., de Carvalho, M.H. Regul. Pept. (2006) [Pubmed]
  12. The kinin system mediates hyperalgesia through the inducible bradykinin B1 receptor subtype: evidence in various experimental animal models of type 1 and type 2 diabetic neuropathy. Gabra, B.H., Berthiaume, N., Sirois, P., Nantel, F., Battistini, B. Biol. Chem. (2006) [Pubmed]
  13. Genomic DNA sequence, expression, and chromosomal localization of the human B1 bradykinin receptor gene BDKRB1. Chai, K.X., Ni, A., Wang, D., Ward, D.C., Chao, J., Chao, L. Genomics (1996) [Pubmed]
  14. In vivo DNase I-mediated footprinting analysis along the human bradykinin B1 receptor (BDKRB1) gene promoter: evidence for cell-specific regulation. Angers, M., Drouin, R., Bachvarova, M., Paradis, I., Bissell, B., Hiromura, M., Usheva, A., Bachvarov, D. Biochem. J. (2005) [Pubmed]
  15. Expression cloning of a human B1 bradykinin receptor. Menke, J.G., Borkowski, J.A., Bierilo, K.K., MacNeil, T., Derrick, A.W., Schneck, K.A., Ransom, R.W., Strader, C.D., Linemeyer, D.L., Hess, J.F. J. Biol. Chem. (1994) [Pubmed]
  16. Spontaneous formation of a proteolytic B1 and B2 bradykinin receptor complex with enhanced signaling capacity. Kang, D.S., Ryberg, K., Mörgelin, M., Leeb-Lundberg, L.M. J. Biol. Chem. (2004) [Pubmed]
  17. Inhibition of human and rabbit arterial smooth muscle cell migration mediated by the kinin B1 receptor: role of receptor density and released mediators. Morissette, G., Sabourin, T., Adam, A., Marceau, F. Can. J. Physiol. Pharmacol. (2006) [Pubmed]
  18. The human B1 bradykinin receptor exhibits high ligand-independent, constitutive activity. Roles of residues in the fourth intracellular and third transmembrane domains. Leeb-Lundberg, L.M., Kang, D.S., Lamb, M.E., Fathy, D.B. J. Biol. Chem. (2001) [Pubmed]
  19. Inhibition of DNA synthesis and growth in human breast stromal cells by bradykinin: evidence for independent roles of B1 and B2 receptors in the respective control of cell growth and phospholipid hydrolysis. Patel, K.V., Schrey, M.P. Cancer Res. (1992) [Pubmed]
  20. High-affinity binding of peptide agonists to the human B1 bradykinin receptor depends on interaction between the peptide N-terminal L-lysine and the fourth extracellular domain of the receptor. Fathy, D.B., Kyle, D.J., Leeb-Lundberg, L.M. Mol. Pharmacol. (2000) [Pubmed]
  21. Tyrosine phosphorylation and activation of pp60c-src and pp125FAK in bradykinin-stimulated fibroblasts. Lee, K.M., Villereal, M.L. Am. J. Physiol. (1996) [Pubmed]
  22. Ligand-induced phosphorylation/dephosphorylation of the endogenous bradykinin B2 receptor from human fibroblasts. Blaukat, A., Alla, S.A., Lohse, M.J., Müller-Esterl, W. J. Biol. Chem. (1996) [Pubmed]
  23. Des-Arg(10)-kallidin engagement of the B1 receptor stimulates type I collagen synthesis via stabilization of connective tissue growth factor mRNA. Ricupero, D.A., Romero, J.R., Rishikof, D.C., Goldstein, R.H. J. Biol. Chem. (2000) [Pubmed]
  24. Bradykinin stimulates IL-6 and IL-8 production by human lung fibroblasts through ERK- and p38 MAPK-dependent mechanisms. Hayashi, R., Yamashita, N., Matsui, S., Fujita, T., Araya, J., Sassa, K., Arai, N., Yoshida, Y., Kashii, T., Maruyama, M., Sugiyama, E., Kobayashi, M. Eur. Respir. J. (2000) [Pubmed]
  25. Kinin B1 receptor expression and function on human brain endothelial cells. Prat, A., Biernacki, K., Pouly, S., Nalbantoglu, J., Couture, R., Antel, J.P. J. Neuropathol. Exp. Neurol. (2000) [Pubmed]
  26. Transcription factor nuclear factor kappaB regulates the inducible expression of the human B1 receptor gene in inflammation. Ni, A., Chao, L., Chao, J. J. Biol. Chem. (1998) [Pubmed]
  27. PGE2 release by bradykinin in human airway smooth muscle cells: involvement of cyclooxygenase-2 induction. Pang, L., Knox, A.J. Am. J. Physiol. (1997) [Pubmed]
  28. B1 kinin receptor does not contribute to vascular tone or tissue plasminogen activator release in the peripheral circulation of patients with heart failure. Cruden, N.L., Tse, G.H., Fox, K.A., Ludlam, C.A., Megson, I., Newby, D.E. Arterioscler. Thromb. Vasc. Biol. (2005) [Pubmed]
  29. Up-regulation of functional kinin B1 receptors in allergic airway inflammation. Christiansen, S.C., Eddleston, J., Woessner, K.M., Chambers, S.S., Ye, R., Pan, Z.K., Zuraw, B.L. J. Immunol. (2002) [Pubmed]
  30. Kinin B1 and B2 receptors are overexpressed in the hippocampus of humans with temporal lobe epilepsy. Perosa, S.R., Arga??araz, G.A., Goto, E.M., Costa, L.G., Konno, A.C., Varella, P.P., Santiago, J.F., Pesquero, J.B., Canzian, M., Amado, D., Yacubian, E.M., Carrete, H., Centeno, R.S., Cavalheiro, E.A., Silva, J.A., Mazzacoratti, M.d.a. .G. Hippocampus (2007) [Pubmed]
  31. Human B1 and B2 bradykinin receptors and their agonists target caveolae-related lipid rafts to different degrees in HEK293 cells. Lamb, M.E., Zhang, C., Shea, T., Kyle, D.J., Leeb-Lundberg, L.M. Biochemistry (2002) [Pubmed]
  32. Kinin B1 receptor antagonists containing alpha-methyl-L-phenylalanine: in vitro and in vivo antagonistic activities. Gobeil, F., Charland, S., Filteau, C., Perron, S.I., Neugebauer, W., Regoli, D. Hypertension (1999) [Pubmed]
WikiGenes - Universities