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Angelica dahurica extract-treated cells showed significant increases in GPR119 activation, intracellular cAMP levels, GLP-1 (zeige GCG ELISA Kits) levels and glucose-stimulated insulin (zeige INS ELISA Kits) secretion as compared with controls
Describe novel small-molecule GPR119 agonists with high receptor selectivity and capacity to induce glucose-stimulated insulin (zeige INS ELISA Kits) secretion.
The GPR119 agonist, HD0471042 increased intracellular cAMP levels in stably human GPR119 expressing CHO cells.
Oxidized-LDL significantly induces lincRNA-DYNLRB2 (zeige DYNLRB2 ELISA Kits)-2 expression, which promotes ABCA1 (zeige ABCA1 ELISA Kits)-mediated cholesterol efflux and inhibits inflammation through GPR119 in THP-1 (zeige GLI2 ELISA Kits) cells.
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.
transfection of GLUTag cells with recombinant human GPR119 results in a constitutive and apparently ligand-independent increase of proglucagon (zeige GCG ELISA Kits) gene promoter activity and proglucagon (zeige GCG ELISA Kits) mRNA content.
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.
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.
Data show that Phe-V:13 can serve as an aromatic lock for the proposed active conformation of the Trp (zeige TBPL1 ELISA Kits)-VI:13 rotameric switch, being involved in the global movement of TM-V and TM-VI in 7TM receptor (zeige CHRM2 ELISA Kits) activation.
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
beta-cell GPR119 expression is dispensable for the physiological control of insulin (zeige INS ELISA Kits) secretion.
we offer evidence for a GPR119-based signaling system in the mammalian eye, with receptors, ligands, and function in the form of a reduction in IOP. Notably this reduction in pressure is restricted to female mice
fat-derived monoacylglycerols are potent candidates for mediating fat-induced GLP-1 (zeige GCG ELISA Kits) release through GPR119 in vivo.
GPR119 in L-cells plays a key role in oral lipid-triggered GLP-1 (zeige GCG ELISA Kits) secretion.
Data indicate that G-protein coupled receptor 119 (GPR119) knockout prevents the therapeutic effects of Gordonoside F.
Novel GPR119 agonist, HD0471042, effectively controlled glucose levels and prevented weight gain in type 2 diabetic mice.
AR231453, a GPR119 agonist, can stimulate beta-cell replication and improve islet graft function
Our results demonstrate that combining a GPR119 agonist with a DPP-IV (zeige DPP4 ELISA Kits) inhibitor may offer a novel therapeutic strategy for stimulating beta-cell regeneration and reversing diabetes.
This gene encodes a member of the rhodopsin subfamily of G-protein-coupled receptors that is expressed in the pancreas and gastrointestinal tract. The encoded protein is activated by lipid amides including lysophosphatidylcholine and oleoylethanolamide and may be involved in glucose homeostasis. This protein is a potential drug target in the treatment of type 2 diabetes.
G protein-coupled receptor 119
, G-protein coupled receptor 2
, glucose-dependent insulinotropic receptor
, G-protein coupled receptor 119