Property Summary

NCBI Gene PubMed Count 93
Grant Count 13
R01 Count 9
Funding $670,886.58
PubMed Score 124.46
PubTator Score 236.75

Knowledge Summary

Patent (8,761)

Expression

MLP Assay (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
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)
743250 screening 1 / 0 / 0 Discovery and characterization of a small molecule allosteric agonists of mas-related G-Protein coupled receptor X1 ( MrgX1)
More...

Gene RIF (77)

PMID Text
25503118 B1R agonist acts as a functional stimulus for the secretion of KLK1 and KLK6, an event relevant for kinin production and cell invasion, respectively
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.
24728914 promotes adhesion of neutrophils to endothelial cells
24686079 APJ and B1R can form heterodimers in transfected HEK293 cells and activations of APJ and B1R could up-regulate eNOS phosphorylation
24475248 A novel B1R splice variant and promoter regulatory elements determine tissue-specific B1R expression.
24401952 BKR1 and BKR2 gene expression on peripheral monocytes is upregulated in essential hypertension
24304135 B1 receptor-mediated vasodilatation in myometrial vessels absent in pre-eclampsia
24108126 CPM binding to extracellular loop 2 of the B1R results in positive allosteric modulation of B1R signaling, and disruption of this interaction could provide a novel therapeutic approach to reduce pathological B1R signaling.
23934212 Bradykinin B1 receptor signaling depends on receptor endocytosis.
23428345 This review focuses on airway MAPK/NFkappaB-dependent kinin receptor upregulation that links the environmental risk factors to airway hyperreactivity and airway inflammation.
More...

AA Sequence

MASSWPPLELQSSNQSQLFPQNATACDNAPEAWDLLHRVLPTFIISICFFGLLGNLFVLLVFLLPRRQLN      1 - 70
VAEIYLANLAASDLVFVLGLPFWAENIWNQFNWPFGALLCRVINGVIKANLFISIFLVVAISQDRYRVLV     71 - 140
HPMASRRQQRRRQARVTCVLIWVVGGLLSIPTFLLRSIQAVPDLNITACILLLPHEAWHFARIVELNILG    141 - 210
FLLPLAAIVFFNYHILASLRTREEVSRTRCGGRKDSKTTALILTLVVAFLVCWAPYHFFAFLEFLFQVQA    211 - 280
VRGCFWEDFIDLGLQLANFFAFTNSSLNPVIYVFVGRLFRTKVWELYKQCTPKSLAPISSSHRKEIFQLF    281 - 350
WRN                                                                       351 - 353
//

Text Mined References (94)

PMID Year Title
25503118 2014 Bioregulation of kallikrein-related peptidases 6, 10 and 11 by the kinin B? receptor in breast cancer cells.
25289859 2015 Downregulation of kinin B1 receptor function by B2 receptor heterodimerization and signaling.
24728914 2015 Kinin B1 receptor regulates interactions between neutrophils and endothelial cells by modulating the levels of Mac-1, LFA-1 and intercellular adhesion molecule-1.
24686079 2014 Heterodimerization of human apelin and bradykinin 1 receptors: novel signal transduction characteristics.
24475248 2014 Novel kinin B? receptor splice variant and 5'UTR regulatory elements are responsible for cell specific B? receptor expression.
24401952 2014 Differential gene expression of bradykinin receptors 1 and 2 in peripheral monocytes from patients with essential hypertension.
24304135 2014 Bradykinin B1 receptor-mediated vasodilation is impaired in myometrial arteries from women with pre-eclampsia.
24108126 2013 Carboxypeptidase M is a positive allosteric modulator of the kinin B1 receptor.
23934212 2014 Kinin-stimulated B1 receptor signaling depends on receptor endocytosis whereas B2 receptor signaling does not.
23597562 2013 Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties.
More...