Bradykinin receptor B1

Identifiers

BDKRB1 ; B1BKR; B1R; BDKRB2; BKB1R; BKR1; BRADYB1

External IDs

OMIM: 600337 MGI: 88144 HomoloGene: 570 IUPHAR: 41 ChEMBL: 4308 GeneCards: BDKRB1 Gene

Gene ontology
Molecular function	• bradykinin receptor activity • protein binding • peptide binding
Cellular component	• endoplasmic reticulum • cytosol • plasma membrane • integral component of plasma membrane • neuron projection
Biological process	• negative regulation of protein phosphorylation • positive regulation of leukocyte migration • inflammatory response • positive regulation of cytosolic calcium ion concentration • protein kinase C-activating G-protein coupled receptor signaling pathway • response to mechanical stimulus • cell migration • sensory perception of pain • negative regulation of cell growth • response to lipopolysaccharide • negative regulation of blood pressure • positive regulation of release of sequestered calcium ion into cytosol
Sources: Amigo / QuickGO

RNA expression pattern

More reference expression data

Orthologs

Species

Human

Mouse

623

RefSeq (mRNA)

RefSeq (protein)

Location (UCSC)

Chr 14:
96.26 – 96.27 Mb

Chr 12:
105.6 – 105.61 Mb

PubMed search

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

References

External links

"Bradykinin Receptors: B₁". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

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. 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. 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.
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. 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.

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3

Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)

Serotonin	(all but 5-HT3) 5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)

Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine (D1 D2 D3 D4 D5) Histamine (H1 H2 H3 H4) Melatonin (1A 1B 1C) TAAR (1 2 3 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 (1 2) FPRL1 OXE Prostaglandin (DP (1 2), EP (1 2 3 4), FP) Prostacyclin Thromboxane

Other	Bile acid Cannabinoid (CB1 CB2, GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Lactate Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Niacin (1 2) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide	B/W (1 2) FF (1 2) S Y (1 2 4 5) Neuromedin (B U (1 2)) Neurotensin (1 2)

Other	Anaphylatoxin (C3a C5a) Angiotensin (1 2) Apelin Bombesin (BRS3 GRPR NMBR) Bradykinin (B1 B2) Chemokine Cholecystokinin (A B) Endothelin (A B) Formyl peptide (1 2 3) FSH Galanin (1 2 3) GHB receptor Gonadotropin-releasing hormone (1 2) Ghrelin Kisspeptin Luteinizing hormone/choriogonadotropin MAS (1 1L D E F G X1 X2 X3 X4) Melanocortin (1 2 3 4 5) MCHR (1 2) Motilin Opioid (Delta Kappa Mu Nociceptin & Zeta, but not Sigma) Orexin (1 2) Oxytocin Prokineticin (1 2) Prolactin-releasing peptide Relaxin (1 2 3 4) Somatostatin (1 2 3 4 5) Tachykinin (1 2 3) Thyrotropin Thyrotropin-releasing hormone Urotensin-II Vasopressin (1A 1B 2)

Miscellaneous

Orphan	GPR (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 77 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)

Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B: Secretin like

Adhesion	ADGRG (1 2 3 4 5 6 7)

Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)

Other	Brain-specific angiogenesis inhibitor (1 2 3) Cadherin (1 2 3) Calcitonin CALCRL CD97 Corticotropin-releasing hormone (1 2) EMR (1 2 3) Glucagon (GR GIPR GLP1R GLP2R) Growth hormone releasing hormone PACAPR1 GPR Latrophilin (1 2 3 ELTD1) Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic glutamate / pheromone

Taste	TAS1R (1 2 3) TAS2R (1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60)

Other	Calcium-sensing receptor GABA B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F: Frizzled / Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)

Smoothened	Smoothened

Neuropeptide receptors

G protein-coupled receptor

Hormone receptors

Hypothalamic	CRH FSH LHRH TRH Somatostatin

Pituitary	Vasopressin 1A 1B 2 Oxytocin LHCG TSH

Other	Atrial natriuretic factor NPR3 Calcitonin Cholecystokinin A B VIP

Opioid receptors

Other neuropeptide receptors

Type I cytokine receptor

GH
Prolactin

Enzyme-linked receptor

Atrial natriuretic factor
- NPR1
- NPR2

Other

Sigma
- 1
- 2

This article is issued from Wikipedia - version of the Wednesday, April 29, 2015. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.

Bradykinin receptor B1

Antagonists

See also

References

External links

Further reading