Cisbio Announces Results of GPCR-Focused Research in Collaboration with IGF

Cisbio Bioassays, a member of IBA group and a global developer of HTRF® (Homogeneous Time-Resolved Fluorescence) technology and services used in assay development and drug screening, has announced findings from its R&D collaboration with the Department of Molecular Pharmacology at the Institute of Functional Genomics (IGF) focused on the structural organization of G-Protein Coupled Receptors (GPCRs).

The results of the collaboration, which describe new methodologies for analyzing receptors at the cell surface of living cells, allow for a better understanding of the spatial structure, mechanisms, and functionality of GPCRs, one of the most important target classes investigated in drug discovery research.

Using a combination of HTRF and SNAP-Tag™ technologies, Cisbio and IGF set up TR-FRET (Time- Resolved Fluorescence Resonance Energy Transfer) assays to demonstrate that GPCRs can adopt a specific organization on the cell surface. These investigations show, in particular, that different class C GPCRs can assemble into either strict dimers or larger oligomers.

TR-FRET, on which HTRF is based, presents numerous advantages over assay technologies such as FRET and BRET (Bioluminescence Resonance Energy Transfer) for analyzing living cells as it offers a higher signal to noise ratio and discriminates between the cell surface protein and the intracellular cell compartment.

The findings illustrate new methods for rapidly and quantitatively analyzing cell surface signaling complexes in living cells in a high throughput format that can potentially be applied to drug screening processes. This improved analysis of cell-to-cell communication can, in turn, facilitate research and discovery of new therapeutics.

Articles detailing the methodologies used were published in two journals, “Functioning of the dimeric GABAB receptor extracellular domain revealed by glycan wedge scanning” in The European Molecular Biology Organization Journal and “Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies: application to GPCR oligomerization” in Nature Methods.

“This latest collaboration is an example of how Cisbio’s R&D expertise in chemistry, technology and biology were combined to bring technical breakthroughs to the GPCR field,” said Eric Trinquet, Head of Technology and Chemistry at Cisbio, who supervised the research. “Our dedication to R&D, innovation and our partnerships with top-notch research institutes like IGF position us at the forefront of GPCR research.”