mProX™ Human GPR119 Stable Cell Line
- Product Category:
- Membrane Protein Stable Cell Lines
- Subcategory:
- GPCR Cell Lines
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Published Data
Fig.1 Effect of GPR119 knockdown on OEA-induced cAMP expression.
mGLUTag cells underwent transfection with either scrambled siRNA (20 pmol/l, control) or GPR119 siRNA (20 pmol/l) 48 hours prior to the experiment. Subsequently, cells were exposed to either medium alone (1% DMSO, negative control) or OEA (10-15 μmol/l) for a duration of 2 hours. The cellular cAMP levels (n = 6) were quantified utilizing RIA.
Ref: Lauffer, Lina M., Roman Iakoubov, and Patricia L. Brubaker. "GPR119 is essential for oleoylethanolamide-induced glucagon-like peptide-1 secretion from the intestinal enteroendocrine L-cell." Diabetes 58.5 (2009): 1058-1066.
Pubmed: 19208912
DOI: 10.2337/db08-1237
Research Highlights
Lee SH, et al. "GPR119 activation by DA-1241 alleviates hepatic and systemic inflammation in MASH ." Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 2023.
The activation of GPR119 has been proposed as a means to improve hyperglycemia, dyslipidemia and hepatic steatosis. However, its efficacy in treating metabolic dysfunction-associated steatohepatitis (MASH) has not been thoroughly explored. In this study, the effects of a novel GPR119 agonist, DA-1241, on MASH were investigated and its underlying anti-inflammatory mechanism was explored. The anti-MASH effect was assessed in various MASH mouse models and changes in NFkappaB signaling were observed in cells. Results showed that DA-1241 effectively attenuated MASH progression and improved MASH symptoms in different etiological models, without glucose-lowering activity. Furthermore, when combined with a dipeptidyl peptidase 4 (DPP4) inhibitor, DA-1241 showed additional improvements in MASH phenotype by enhancing endogenous glucagon-like peptide-1 effects. It also reduced liver inflammation and restored hepatic gene expression, leading to reduced systemic inflammation. These findings suggest the therapeutic potential of DA-1241, both alone and in combination with a DPP4 inhibitor, for the treatment of MASH.
Pubmed:
37657264
DOI:
10.1016/j.biopha.2023.115345
Korkus E, et al. "Trans-palmitoleic acid, a dairy fat biomarker, stimulates insulin secretion and ." Food & function, 2023.
The study investigated the effects of two polyunsaturated fatty acid (POA) isomers, tPOA and cPOA, on insulin secretion in murine and human pancreatic beta cell lines. It also examined their ability to activate specific G protein-coupled receptors proposed as potential targets for treating type 2 diabetes mellitus (T2DM). Results showed that both isomers enhanced glucose-stimulated insulin secretion, but through different signaling pathways. Molecular simulations were also conducted to predict the binding strength between the isomers and selected receptors. This study provides valuable insight into the potential of POA isomers as regulators of glucose homeostasis and their ability to promote insulin secretion through GPCR activation.
Pubmed:
37368452
DOI:
10.1039/d2fo03412c