Cellular models for GPCR drug evaluation

news July 26 2022

G-Protein Coupled Receptors (GPCRs) are a large family of proteins involved in a myriad of biological processes. They represent important therapeutic targets: approximately 50% of existing drugs target a GPCR. However, they have traditionally been difficult targets to evaluate in vitro. BPS Bioscience has developed cell lines to elucidate their biological function or for drug screening and characterization.

  • GLP1R/CRE and CGRPR/CRE luciferase cell lines (conditional reporter)
  • Adenosine A2A Receptor: functional receptor stably expressed in HEK293 cells
  • Monkey and human GPRC5D overexpressing cells

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Glucagon-like Peptide 1 Receptor (GLP-1R)

GLP-1R is expressed in pancreatic β cells and is activated by the peptide hormone glucagon-like peptide 1 (GLP-1) secreted from intestinal cells after nutrient intake. GLP-1R regulates blood sugar levels by enhancing glucose-stimulated insulin secretion. It is a therapeutic target for the treatment of diabetes, with several

FDA-approved GLP-1 agonists currently used in the clinic.

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