Property Summary

NCBI Gene PubMed Count 24
PubMed Score 103.13
PubTator Score 75.68

Knowledge Summary

Patent (44,794)

TINX Plot

  Disease Sources (1)

Disease Target Count Z-score Confidence
diabetes mellitus 1663 4.316 2.2
Obesity 616 3.074 1.5

Synonym

Accession Q8TDV5 Q495H7 Q4VBN3
Symbols GPCR2

Gene

PANTHER Protein Class (2)

  Ortholog (12)

Species Source
Chimp OMA EggNOG
Macaque OMA EggNOG Inparanoid
Mouse OMA EggNOG Inparanoid
Rat OMA Inparanoid
Dog OMA EggNOG Inparanoid
Horse OMA EggNOG Inparanoid
Cow OMA EggNOG Inparanoid
Pig OMA EggNOG
Opossum OMA EggNOG Inparanoid
Chicken OMA EggNOG Inparanoid
Anole lizard OMA EggNOG Inparanoid
Zebrafish OMA EggNOG

  TechDev Info (1)

Gene RIF (10)

PMID Text
24681896 Describe novel small-molecule GPR119 agonists with high receptor selectivity and capacity to induce glucose-stimulated insulin secretion.
24493833 Oxidized-LDL significantly induces lincRNA-DYNLRB2-2 expression, which promotes ABCA1-mediated cholesterol efflux and inhibits inflammation through GPR119 in THP-1 cells.
23897163 The GPR119 agonist, HD0471042 increased intracellular cAMP levels in stably human GPR119 expressing CHO cells.
23798572 transfection of GLUTag cells with recombinant human GPR119 results in a constitutive and apparently ligand-independent increase of proglucagon gene promoter activity and proglucagon mRNA content.
23648181 Replacement of the three methyl groups in 1 with metabolically stable moieties led to the identification of compound 34, a potent and efficacious GPR119 agonist with improved pharmacokinetic (PK) properties.
23069642 Data suggest that GPR119 activation/up-regulation in skeletal muscle impairs fatty acid and glucose oxidation; diet-induced obesity appears to up-regulate skeletal muscle GPR119.
22883930 Results provide evidence of an islet-gastrointestinal distribution of GPR119, its expression in pancreatic beta and alpha cells, and its possible involvement in islet function.
19920139 Data show that Phe-V:13 can serve as an aromatic lock for the proposed active conformation of the Trp-VI:13 rotameric switch, being involved in the global movement of TM-V and TM-VI in 7TM receptor activation.
19901198 findings show that N-oleoyldopamine (OLDA)& structurally related hydroxybenzyl amides are robust activators of GPR119; studies indicate that multiple, distinct classes of lipid amides, acting via GPR119, may be important modulators of glucose homeostasis
16517404 GPR119 therefore represents a novel and attractive potential target for the therapy of obesity and related metabolic disorders.

AA Sequence

MESSFSFGVILAVLASLIIATNTLVAVAVLLLIHKNDGVSLCFTLNLAVADTLIGVAISGLLTDQLSSPS      1 - 70
RPTQKTLCSLRMAFVTSSAAASVLTVMLITFDRYLAIKQPFRYLKIMSGFVAGACIAGLWLVSYLIGFLP     71 - 140
LGIPMFQQTAYKGQCSFFAVFHPHFVLTLSCVGFFPAMLLFVFFYCDMLKIASMHSQQIRKMEHAGAMAG    141 - 210
GYRSPRTPSDFKALRTVSVLIGSFALSWTPFLITGIVQVACQECHLYLVLERYLWLLGVGNSLLNPLIYA    211 - 280
YWQKEVRLQLYHMALGVKKVLTSFLLFLSARNCGPERPRESSCHIVTISSSEFDG                   281 - 335
//

Text Mined References (25)

PMID Year Title
24681896 2014 Discovery and characterization of novel small molecule agonists of G protein-coupled receptor 119.
24493833 2014 A lincRNA-DYNLRB2-2/GPR119/GLP-1R/ABCA1-dependent signal transduction pathway is essential for the regulation of cholesterol homeostasis.
23897163 2014 Novel GPR119 agonist HD0471042 attenuated type 2 diabetes mellitus.
23798572 2013 Stimulation of proglucagon gene expression by human GPR119 in enteroendocrine L-cell line GLUTag.
23648181 2013 Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists.
23382219 2013 Structural basis for endosomal trafficking of diverse transmembrane cargos by PX-FERM proteins.
23069642 2013 GPR119 regulates genetic markers of fatty acid oxidation in cultured skeletal muscle myotubes.
22883930 2013 GPR119 expression in normal human tissues and islet cell tumors: evidence for its islet-gastrointestinal distribution, expression in pancreatic beta and alpha cells, and involvement in islet function.
19920139 2010 A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors.
19901198 2010 N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119.
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