| Tclin | B2 bradykinin receptor |
This gene encodes a receptor for bradykinin. The 9 aa bradykinin peptide elicits many responses including vasodilation, edema, smooth muscle spasm and pain fiber stimulation. This receptor associates with G proteins that stimulate a phosphatidylinositol-calcium second messenger system. Alternate start codons result in two isoforms of the protein. [provided by RefSeq, Jul 2008]
Comments
| Disease | log2 FC | p |
|---|---|---|
| malignant mesothelioma | -4.700 | 0.000 |
| cystic fibrosis | 3.435 | 0.000 |
| lung cancer | -1.600 | 0.001 |
| group 4 medulloblastoma | -1.100 | 0.002 |
| lung adenocarcinoma | 1.500 | 0.000 |
| invasive ductal carcinoma | -1.299 | 0.032 |
CHEMBL209130
pKi 7.00
CHEMBL207465
pKi 7.00
CHEMBL267822
pKi 7.00
CHEMBL3215541
pIC50 7.01
CHEMBL1907652
pKi 7.02
CHEMBL295005
pIC50 7.03
CHEMBL27702
pKi 7.04
CHEMBL561899
pIC50 7.05
CHEMBL3215529
pIC50 7.06
CHEMBL3350763
pKi 7.07
CHEMBL295428
pIC50 7.10
CHEMBL550143
pIC50 7.10
CHEMBL210100
pKi 7.10
CHEMBL380206
pKi 7.10
CHEMBL159066
pKi 7.10
CHEMBL542911
pIC50 7.11
CHEMBL26192
pKi 7.12
CHEMBL26847
pKi 7.13
CHEMBL130660
pIC50 7.13
CHEMBL286556
pKi 7.14
| AID | Type | Active / Inconclusive / Inactive | Description |
|---|---|---|---|
| 1788 | other |
0 / 0 / 0 | Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity |
| 1921 | other |
2 / 0 / 0 | Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator: Ancillary Activity |
| 624355 | other |
0 / 0 / 0 | Late stage results from the probe development efforts to identify dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and nuclear factor NF-kappa-B (NF-kB): Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs |
| 624406 | other |
0 / 0 / 0 | Late stage results from the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs |
| 652083 | other |
0 / 0 / 0 | Late-stage results from the probe development effort to identify antagonists of OPRK1: CEREP radiometric-based biochemical counterscreen panel assay |
| 686924 | other |
0 / 0 / 1 | ML347 Eurofin Panel Assay for BMP Inhibitor (Probe Compound) |
| 686925 | other |
0 / 0 / 1 | ML352 Eurofin Panel Assay for Choline Transporter Inhibitor (Probe Compound) |
| 686926 | other |
0 / 0 / 1 | ML354 Eurofin Panel Assay for PAR4 Antagonists Inhibitor (Probe Compound) |
| 686927 | other |
0 / 0 / 1 | ML353 Eurofin Panel Assay for mGlu5 SAM Inhibitor (Probe Compound) |
| 743249 | screening |
1 / 0 / 0 | Development of the First Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator (NAM) |
| More... |
| PMID | Text |
|---|---|
| 26907838 | These results suggest that the response to long-term exercise training could be modulated by the BDKRB2 gene -9/+9 polymorphism in male athletes. In well-trained swimmers, BDKRB2 gene variation was not found to be an independent determinant of swimming performance. |
| 26362411 | Significant association between the -58T/C polymorphism and the increased risk of Hypertension was found in Northern Han Chinese population. |
| 26360782 | Bradykinin inhibits oxidative stress-induced senescence of endothelial progenitor cells through the B2R/AKT/RB and B2R/EGFR/RB signal pathways. |
| 26235941 | A cross-talk was found between bradykinin B2 receptor and cytokines in retinal pigment epithelium. |
| 25970620 | The nasal mucosa specimens from chronic rhinosinusitis patients expressed relatively higher B2R and slightly higher kininogen (KNG)/BK and B1R. |
| 25842860 | Bradykinin receptor B2-VNTR length polymorphism was not associated with angina pectoris and myocardial infarction in Russian men. |
| 25713410 | These results indicate that B2R couples with P2Y2R and that these G-protein-coupled receptors act together to fine-tune cellular responsiveness. |
| 25641172 | Bradykinin receptor B2 (B2R) genetic variation may affect thirst because of effects bradykinin activity. |
| 25529519 | Genetic variation was observed in obese patients with hypertension, obese patients' total cholesterol levels varied by genotype, and waist circumference and blood pressure were elevated in the non-obese having a C/C genotype compared to T/C and T/T. |
| 25289859 | kB1R heterodimerizes with kB2Rs in co-transfected HEK293 cells and natively expressing endothelial cells, resulting in significant internalization and desensitization of the kB1R response in cells pre-treated with kB2R agonist. |
| More... |
MFSPWKISMFLSVREDSVPTTASFSADMLNVTLQGPTLNGTFAQSKCPQVEWLGWLNTIQPPFLWVLFVL 1 - 70 ATLENIFVLSVFCLHKSSCTVAEIYLGNLAAADLILACGLPFWAITISNNFDWLFGETLCRVVNAIISMN 71 - 140 LYSSICFLMLVSIDRYLALVKTMSMGRMRGVRWAKLYSLVIWGCTLLLSSPMLVFRTMKEYSDEGHNVTA 141 - 210 CVISYPSLIWEVFTNMLLNVVGFLLPLSVITFCTMQIMQVLRNNEMQKFKEIQTERRATVLVLVVLLLFI 211 - 280 ICWLPFQISTFLDTLHRLGILSSCQDERIIDVITQIASFMAYSNSCLNPLVYVIVGKRFRKKSWEVYQGV 281 - 350 CQKGGCRSEPIQMENSMGTLRTSISVERQIHKLQDWAGSRQ 351 - 391 //
| PMID | Year | Title |
|---|---|---|
| 26907838 | 2016 | Effect of BDKRB2 Gene -9/+9 Polymorphism on Training Improvements in Competitive Swimmers. |
| 26362411 | 2016 | Association of the bradykinin receptors genes variants with hypertension: a case-control study and meta-analysis. |
| 26360782 | 2015 | Bradykinin inhibits oxidative stress-induced senescence of endothelial progenitor cells through the B2R/AKT/RB and B2R/EGFR/RB signal pathways. |
| 26235941 | 2015 | Enhanced Ca(2+) response and stimulation of prostaglandin release by the bradykinin B2 receptor in human retinal pigment epithelial cells primed with proinflammatory cytokines. |
| 25970620 | 2015 | Involvement of B2 receptor in bradykinin-induced proliferation and proinflammatory effects in human nasal mucosa-derived fibroblasts isolated from chronic rhinosinusitis patients. |
| 25842860 | [[Length polymorphism of minisatellite repeat B2-VNTR of the bradykinin B2 receptor gene in healthy Russians and in patients with coronary heart disease]. | |
| 25713410 | 2015 | Close association of B2 bradykinin receptors with P2Y2 ATP receptors. |
| 25641172 | 2015 | The influence of angiotensin converting enzyme and bradykinin receptor B2 gene variants on voluntary fluid intake and fluid balance in healthy men during moderate-intensity exercise in the heat. |
| 25529519 | 2014 | The relationship of Bradykinin B? receptor gene variation with obesity, hypertension and lipid variables in obese patients. |
| 25289859 | 2015 | Downregulation of kinin B1 receptor function by B2 receptor heterodimerization and signaling. |
| More... |
