Property Summary

NCBI Gene PubMed Count 24
Grant Count 9
R01 Count 3
Funding $681,886.4
PubMed Score 103.13
PubTator Score 75.68

Knowledge Summary

Patent (44,794)

TINX Plot

  Disease Relevance (2)

Disease Z-score Confidence
diabetes mellitus 1,663 4.316 2.2
Obesity 616 3.074 1.5

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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