Property Summary

NCBI Gene PubMed Count 116
Grant Count 45
R01 Count 22
Funding $7,278,458.8
PubMed Score 246.07
PubTator Score 344.88

Knowledge Summary

Patent (1,223)

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)
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Gene RIF (83)

PMID Text
26817839 Cell surface ubiquitination precedes endocytosis, after which USP14 acts as an ubiquitin-binding protein that targets the ubiquitinated GABA B receptor to lysosomal degradation and promotes its deubiquitination.
26727527 Results show that GABBR1 minor genotypes/alleles were protective against risk for alcoholism in 3 ethnically diverse cohorts.
25725285 GABA(B)R stimulation promotes chemotaxis in RBL cells which is dependent on signaling via PI3-K/Akt, Src kinases and on rearrangement of both microtubules and actin cytoskeleton.
25465316 the first report of abnormal levels of GABA+ and Glx in mood-related brain regions of women with PMDD, indicating that dysregulation of the amino acid neurotransmitter system may be an important neurobiological mechanism in the pathogenesis of PMDD.
24778228 The endoplasmic reticulum retention signal of GBR1 is not part of the core coiled-coil structure, suggesting that it is sterically shielded by GBR2 upon heterodimer formation.
24682435 GABBR1 receptors are expressed in aortic smooth muscle cells and regulate the [Ca(2+)]i via a Gi/o-coupled receptor pathway and a phospholipase C activation pathway.
24209778 Chronic alcohol altered exon/intron expression and splice junction levels.
24006265 GABBR1 protein involved in phenylthiourea bitter taste detection.
23391219 Authors suggest GABBR1, GABA receptor B1, is implicated in schizophrenia based on a Human endogenous retrovirus long terminal repeat (HERV-W LTR) in the regulatory region of GABBR1.
23192081 Activation of GABA(B) receptors significantly inhibits Akt/GSK-3 signaling in a beta-arrestin-dependent pathway.
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AA Sequence

MLLLLLLAPLFLRPPGAGGAQTPNATSEGCQIIHPPWEGGIRYRGLTRDQVKAINFLPVDYEIEYVCRGE      1 - 70
REVVGPKVRKCLANGSWTDMDTPSRCVRICSKSYLTLENGKVFLTGGDLPALDGARVDFRCDPDFHLVGS     71 - 140
SRSICSQGQWSTPKPHCQVNRTPHSERRAVYIGALFPMSGGWPGGQACQPAVEMALEDVNSRRDILPDYE    141 - 210
LKLIHHDSKCDPGQATKYLYELLYNDPIKIILMPGCSSVSTLVAEAARMWNLIVLSYGSSSPALSNRQRF    211 - 280
PTFFRTHPSATLHNPTRVKLFEKWGWKKIATIQQTTEVFTSTLDDLEERVKEAGIEITFRQSFFSDPAVP    281 - 350
VKNLKRQDARIIVGLFYETEARKVFCEVYKERLFGKKYVWFLIGWYADNWFKIYDPSINCTVDEMTEAVE    351 - 420
GHITTEIVMLNPANTRSISNMTSQEFVEKLTKRLKRHPEETGGFQEAPLAYDAIWALALALNKTSGGGGR    421 - 490
SGVRLEDFNYNNQTITDQIYRAMNSSSFEGVSGHVVFDASGSRMAWTLIEQLQGGSYKKIGYYDSTKDDL    491 - 560
SWSKTDKWIGGSPPADQTLVIKTFRFLSQKLFISVSVLSSLGIVLAVVCLSFNIYNSHVRYIQNSQPNLN    561 - 630
NLTAVGCSLALAAVFPLGLDGYHIGRNQFPFVCQARLWLLGLGFSLGYGSMFTKIWWVHTVFTKKEEKKE    631 - 700
WRKTLEPWKLYATVGLLVGMDVLTLAIWQIVDPLHRTIETFAKEEPKEDIDVSILPQLEHCSSRKMNTWL    701 - 770
GIFYGYKGLLLLLGIFLAYETKSVSTEKINDHRAVGMAIYNVAVLCLITAPVTMILSSQQDAAFAFASLA    771 - 840
IVFSSYITLVVLFVPKMRRLITRGEWQSEAQDTMKTGSSTNNNEEEKSRLLEKENRELEKIIAEKEERVS    841 - 910
ELRHQLQSRQQLRSRRHPPTPPEPSGGLPRGPPEPPDRLSCDGSRVHLLYK                       911 - 961
//

Text Mined References (116)

PMID Year Title
26817839 2016 Post-endocytotic Deubiquitination and Degradation of the Metabotropic ?-Aminobutyric Acid Receptor by the Ubiquitin-specific Protease 14.
26727527 2016 GABBR1 and SLC6A1, Two Genes Involved in Modulation of GABA Synaptic Transmission, Influence Risk for Alcoholism: Results from Three Ethnically Diverse Populations.
25725285 2015 Cytoskeletal rearrangement and Src and PI-3K-dependent Akt activation control GABA(B)R-mediated chemotaxis.
25465316 2015 Alterations of GABA and glutamate-glutamine levels in premenstrual dysphoric disorder: a 3T proton magnetic resonance spectroscopy study.
24778228 2014 Heterodimeric coiled-coil interactions of human GABAB receptor.
24682435 2015 GABAB receptors are expressed in human aortic smooth muscle cells and regulate the intracellular Ca(2+) concentration.
24658140 2014 The mammalian-membrane two-hybrid assay (MaMTH) for probing membrane-protein interactions in human cells.
24305054 2013 Structural mechanism of ligand activation in human GABA(B) receptor.
24209778 2014 Altered gamma-aminobutyric acid type B receptor subunit 1 splicing in alcoholics.
24006265 2013 A novel human receptor involved in bitter tastant detection identified using Dictyostelium discoideum.
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