mProX™ Human GLP2R Stable Cell Line
- Product Category:
- Membrane Protein Stable Cell Lines
- Subcategory:
- GPCR Cell Lines
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Published Data
Fig.1 GLP2R expression.
The parental cell line saw an elevation in GLP2R expression through the introduction of overexpression plasmids, denoted as PC-GLP2R-OV or HCC287-GLP2R-OV, via transfection techniques.
Ref: Song, Bin, et al. "GLP2-GLP2R signal affects the viability and EGFR-TKIs sensitivity of PC9 and HCC827 cells." BMC Pulmonary Medicine 22.1 (2022): 1-8.
Pubmed: 35027025
DOI: 10.1186/s12890-021-01800-3
Research Highlights
Valiente PA, et al. "Computational Design of Potent and Selective d-Peptide Agonists of the ." Journal of medicinal chemistry, 2023.
In this study, three d-GLP-2 agonists were developed to specifically activate the glucagon-like peptide-2 receptor (GLP-2R) and increase cyclic adenosine monophosphate (cAMP) accumulation, without stimulating the glucagon-like peptide-1 receptor (GLP-1R). In vitro experiments showed that all three d-GLP-2 agonists increased the expression of phosphorylated protein kinase B (p-AKT) in a time- and concentration-dependent manner. The most effective d-GLP-2 analogue showed a 2.28-fold increase in p-AKT levels compared to the natural l-GLP-2. This enhancement in p-AKT levels could be attributed to the d-GLP-2 agonists' longer activation of GLP-2R and lower recruitment of beta-arrestin. Additionally, these d-GLP-2 agonists have higher stability against protease degradation, indicating potential applications in improving intestinal absorption and treating inflammatory bowel disease, potentially at lower dosages compared to current treatments.
Pubmed:
37491005
DOI:
10.1021/acs.jmedchem.3c00464
Gibadullin R, et al. "Differential Responses of the GLP-1 and GLP-2 Receptors to N-Terminal ." Journal of the American Chemical Society, 2023.
Class B1 G protein-coupled receptors (GPCRs) have a crucial role in detecting extracellular polypeptide agonists and transmitting their messages to the cell's interior. These receptors need to be able to change their shape in response to agonists, and recent research has shown that the mobility of agonists themselves can impact receptor activation. By studying the GLP-2R receptor and comparing it with the GLP-1R receptor, scientists have discovered that variations in the alpha-helical structure of agonists can have different effects on the two receptors. This knowledge could aid in the development of hormone analogues with unique activity profiles, such as a newly discovered GLE analogue that acts as both a potent agonist of the GLP-2R and a potent antagonist of the GLP-1R, demonstrating a novel form of polypharmacology.
Pubmed:
37235770
DOI:
10.1021/jacs.3c01628