Diabetes Research
Gain insight into diabetes disease mechanisms and receptor pharmacology with bright fluorescent biosensor assays. Examine Biased agonism at the GLP-1 and GCGR receptors in cell models and GPCR second messenger signaling in pancreatic islet cells.
GPCR Signaling in Diabetes
Monitor GPCR second messenger signaling kinetics with live-cell, fluorescent GPCR assays. Green and red fluorescent biosensor assays can be combined to detect simultaneous signaling in the same cells or wells. Co-transduce GPCRs like the GLP-1 receptor (#Z0600N), GIP receptor (#Z1600N), and Glucagon receptor (#Z2000N) in cell models of diabetes. Monitor bright fluorescent assay signals on automated plate readers or imaging systems.
Dose-dependent cAMP responses in HEK293 cells co-expressing GLP-1 receptor.
Expression in Pancreatic Islet Cells
Use assay-ready BacMam vectors to express fluorescent biosensors in pancreatic islets and image signaling kinetics. Target expression to specific cell sub-populations with custom promoters. Alternate viral vectors (AV, Lentivirus, AAV) are available by special order as well.
See example research utilizing our assays in pancreatic cell types below:
Pancreatic Cell References
Primary Cultures
Pancreatic Islets (Human)
- N. Zaïmia, et al. GLP-1 and GIP receptors signal through distinct β-arrestin 2-dependent pathways to regulate pancreatic β cell function. Cell Reports. October 2023.
- J. Cho, et al. Islet primary cilia motility controls insulin secretion. Science Advances. September 2022. (bioRxiv)
- J. Almaça, et al. Human beta cells produce and release serotonin to inhibit glucagon secretion from alpha cells.Cell Reports, Volume 17, Issue 12, 2016.
Pancreatic Islets (Mouse)
- A. Oqua, et al. Molecular mapping and functional validation of GLP-1R cholesterol binding sites in pancreatic beta cells. bioRxiv. June 2024.
- C. Hinds, et al. Abolishing β-arrestin recruitment is necessary for the full metabolic benefits of G protein-biased glucagon-like peptide-1 receptor agonists. Diabetes, Obesity and Metabolism. October 2023.
- N. Zaïmia, et al. GLP-1 and GIP receptors signal through distinct β-arrestin 2-dependent pathways to regulate pancreatic β cell function. Cell Reports. October 2023.
- S. Bitsi, et al. Divergent acute versus prolonged pharmacological GLP-1R responses in adult β cell–specific β-arrestin 2 knockout mice. Science Advances. May 2023.
- S. Bitsi, et al. Divergent acute versus prolonged in vivo GLP-1R responses in β-arrestin 2-deleted primary beta cells. bioRxiv. April 2022.
- A. Kim, et al. Arginine-vasopressin mediates counter-regulatory glucagon release and is diminished in type 1 diabetes. eLife. November 2021. (bioRxiv)
- M. Draper, et al. Imaging Meets Cytometry: Analyzing Heterogenous Functional Microscopic Data from Living Cell Populations. J. Imaging. January 2021.
- N. Daram, et al. Glucagon-like Peptide 1 Shows Glucose Dependence in Regulating Islet Hormone Secretion. Metabolism. March 2020.
- M. Marasco et al. Interleukin-6 Reduces b-Cell Oxidative Stress by Linking Autophagy With the Antioxidant Response. Diabetes. August 2018.
- A. Hamilton et al. Adrenaline Stimulates Glucagon Secretion by Tpc2-Dependent Ca2+ Mobilization From Acidic Stores in Pancreatic α-Cells. Diabetes. June 2018.
- M. Shigeto, et al. GLP-1 stimulates insulin secretion by PKC-dependent TRPM4 and TRPM5 activation. J Clinical Invest. 2015. doi:10.1172/JCI81975.
α-Cells (Mouse)
- J. Knudsen, et al. Dysregulation of Glucagon Secretion by Hyperglycemia-Induced Sodium-Dependent Reduction of ATP Production. Cell Metabolism. February 2019.
Cell Lines
EndoC-βH5 (β-cell model)
- C. Hinds, et al. Abolishing β-arrestin recruitment is necessary for the full metabolic benefits of G protein-biased glucagon-like peptide-1 receptor agonists. Diabetes, Obesity and Metabolism. October 2023.
INS-1 (GRINCH)
- C. Amos, et al. Membrane lipids couple synaptotagmin to SNARE-mediated granule fusion in insulin-secreting cells. Molecular Biology of the Cell. December 2023.
INS-1 832 (3 insulinoma cells25)
- Y. Manchange, et al. Engineered mini-G proteins block the internalization of cognate GPCRs and disrupt downstream intracellular signaling. Science Signaling. July 2024.
- A. Oqua, et al. Molecular mapping and functional validation of GLP-1R cholesterol binding sites in pancreatic beta cells. bioRxiv. June 2024.
- G. Austin, et al. An inter-organelle contact between endosomal GLP-1R, ER VAP-B, and the mitochondrial AKAP SPHKAP triggers PKA-dependent MIC19 phosphorylation and β-cell mitochondrial remodelling. bioRxiv. April 2024.
- C. Hinds, et al. Abolishing β-arrestin recruitment is necessary for the full metabolic benefits of G protein-biased glucagon-like peptide-1 receptor agonists. Diabetes, Obesity and Metabolism. October 2023.
MIN6
- C. Wu, et al. Discovery of ciliary G protein-coupled receptors regulating pancreatic islet insulin and glucagon secretion. Genes & Development. August 2021. bioRxiv.
- Q. Wang, et al. Regulator of G protein signaling Gβ5-R7 is a crucial activator of muscarinic M3 receptor-stimulated insulin secretion. FASEB J. Jul. 7,2017.
α-TC9
- C. Wu, et al. Discovery of ciliary G protein-coupled receptors regulating pancreatic islet insulin and glucagon secretion. Genes & Development. August 2021. bioRxiv.
BacMam-mediated cADDis cAMP Sensor expression in a pancreatic islet. Shigeto, et al. 2016.
GLP-1R and GCGR Arrestin Recruitment
Two GPCRs relevant to diabetes signaling pathways – GLP-1R and GCGR – are now available as Borealis arrestin kits! Use cADDis cAMP and Borealis arrestin assays to examine receptor pharmacology in cell models.
Borealis Arrestin GLP-1 receptor kits include the Green fluorescent arrestin sensor, GLP-1R, and GRK 5 packaged in BacMam.
Borealis Arrestin Glucagon receptor kits include Green fluorescent arrestin sensor and GCGR packaged in BacMam.
Gain pharmacological insights from the kinetic data provided by these assays by using Pharmechanics’ Time Course Tool Pack.
Dose-dependent arrestin recruitment data collected by the Borealis Arrestin sensor in HEK 293T cells.
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Contact Us
If you have any questions about using these tools in your cells or would like to request a quote, send us an email at info@montanamolecular.com. We’re happy to help!
