Bradykinin receptor B1 explained

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.

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.^[1]

Classical agonist of this receptor includes bradykinin1-8 (bradykinin with the first 8 amino acid) and antagonist includes [Leu8]-bradykinin1-8.^[2]

Antagonists

• LF22-0542

See also

• Bradykinin receptor

External links

• Web site: Bradykinin Receptors: B₁ . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology . 2008-11-25 . 2016-03-03 . https://web.archive.org/web/20160303193034/http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2975 . dead .

Further reading

• Duchene J, Lecomte F, Ahmed S, Cayla C, Pesquero J, Bader M, Perretti M, Ahluwalia A . A novel inflammatory pathway involved in leukocyte recruitment: role for the kinin B1 receptor and the chemokine CXCL5. . J. Immunol. . 179 . 7 . 4849–56 . 2007 . 17878384 . 10.4049/jimmunol.179.7.4849. 3696729 .
• Calixto JB, Medeiros R, Fernandes ES . Kinin B1 receptors: key G-protein-coupled receptors and their role in inflammatory and painful processes . Br. J. Pharmacol. . 143 . 7 . 803–18 . 2005 . 15520046 . 10.1038/sj.bjp.0706012 . 1575942 . etal.
• Menke JG, Borkowski JA, Bierilo KK . Expression cloning of a human B1 bradykinin receptor . J. Biol. Chem. . 269 . 34 . 21583–6 . 1994 . 10.1016/S0021-9258(17)31844-6 . 8063797 . etal. free .
• Yang X, Polgar P . Genomic structure of the human bradykinin B1 receptor gene and preliminary characterization of its regulatory regions . Biochem. Biophys. Res. Commun. . 222 . 3 . 718–25 . 1996 . 8651911 . 10.1006/bbrc.1996.0810 . free .
• Bachvarov DR, Hess JF, Menke JG . Structure and genomic organization of the human B1 receptor gene for kinins (BDKRB1) . Genomics . 33 . 3 . 374–81 . 1996 . 8660997 . 10.1006/geno.1996.0213 . etal.
• Chai KX, Ni A, Wang D . Genomic DNA sequence, expression, and chromosomal localization of the human B1 bradykinin receptor gene BDKRB1 . Genomics . 31 . 1 . 51–7 . 1996 . 8808279 . 10.1006/geno.1996.0008 . etal. free .
• Leeb T, Mathis SA, Leeb-Lundberg LM . 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 . 1997 . 8995263 . 10.1074/jbc.272.1.311 . free .
• Blaukat A, Herzer K, Schroeder C . Overexpression and functional characterization of kinin receptors reveal subtype-specific phosphorylation . Biochemistry . 38 . 4 . 1300–9 . 1999 . 9930991 . 10.1021/bi981727r . etal.
• Cassano G, Susca F, Lippe C, Guanti G . 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 . 1999 . 10188626 . 10.1016/S0306-3623(98)00275-4 .
• Zhou X, Prado GN, Chai M . 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 . 2000 . 10329474 . 10.1006/mcbr.1999.0105 . etal. free .
• Jones C, Phillips E, Davis C . Molecular characterisation of cloned bradykinin B1 receptors from rat and human . Eur. J. Pharmacol. . 374 . 3 . 423–33 . 1999 . 10422787 . 10.1016/S0014-2999(99)00315-5 . etal.
• Sjuve R, Boels PJ, Uvelius B, Arner A . Up-regulation of bradykinin response in rat and human bladder smooth muscle . J. Urol. . 164 . 5 . 1757–63 . 2000 . 11025765 . 10.1016/S0022-5347(05)67102-9 .
• Sawant S, Snyman C, Bhoola K . Comparison of tissue kallikrein and kinin receptor expression in gastric ulcers and neoplasms . Int. Immunopharmacol. . 1 . 12 . 2063–80 . 2002 . 11710536 . 10.1016/S1567-5769(01)00118-7 .
• Ignjatovic T, Tan F, Brovkovych V . Novel mode of action of angiotensin I converting enzyme inhibitors: direct activation of bradykinin B1 receptor . J. Biol. Chem. . 277 . 19 . 16847–52 . 2002 . 11880373 . 10.1074/jbc.M200355200 . etal. free .
• Newton R, Eddleston J, ((Haddad el-B)) . Regulation of kinin receptors in airway epithelial cells by inflammatory cytokines and dexamethasone . Eur. J. Pharmacol. . 441 . 3 . 193–202 . 2002 . 12063092 . 10.1016/S0014-2999(01)01624-7 . etal.
• Kang DS, Leeb-Lundberg LM . 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 . 2002 . 12130679 . 10.1124/mol.62.2.281 . 86826886 .
• Christiansen SC, Eddleston J, Woessner KM . Up-regulation of functional kinin B1 receptors in allergic airway inflammation . J. Immunol. . 169 . 4 . 2054–60 . 2002 . 12165532 . 10.4049/jimmunol.169.4.2054. etal. free .
• Lamb ME, Zhang C, Shea T . 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 . 2003 . 12450400 . 10.1021/bi020231d . etal.
• Strausberg RL, Feingold EA, Grouse LH . 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 . 2003 . 12477932 . 10.1073/pnas.242603899 . 139241 . 2002PNAS...9916899M . etal. free .
• Kang DS, Ryberg K, Mörgelin M, Leeb-Lundberg LM . Spontaneous formation of a proteolytic B1 and B2 bradykinin receptor complex with enhanced signaling capacity . J. Biol. Chem. . 279 . 21 . 22102–7 . 2004 . 15033977 . 10.1074/jbc.M402572200 . free .
• Gerhard DS, Wagner L, Feingold EA . The Status, Quality, and Expansion of the NIH Full-Length cDNA Project: The Mammalian Gene Collection (MGC) . Genome Res. . 14 . 10B . 2121–7 . 2004 . 15489334 . 10.1101/gr.2596504 . 528928 . etal.

Notes and References

1. Web site: Entrez Gene: BDKRB1 bradykinin receptor B1.
2. Bradykinin receptors in mouse and rat isolated superior cervical ganglia. . 7670739 . 115 . 1908315 . Br J Pharmacol . 368–72 . Seabrook GR, Bowery BJ, Hill RG . 1995 . 2 . 10.1111/j.1476-5381.1995.tb15887.x.