Tag-lite® internalization service
Universal GPCR internalization assay
Cisbio Bioassays offers a comprehensive GPCR platform covering all the GPCR activation pathway, with ligand binding assays, and functional assays including internalization.
All these assays have been developed with the HTRF® technology to investigate and screen drugs.
Tag-lite internalization means G-protein and beta-arrestin-independent assays streamlined to investigate and screen agonist and antagonist and to perform GPCR kinetic internalization assays.
- Compatible with fresh or frozen cells
- Cell-based functional assay
- Miniaturization down to 20µl
- HTRF technology
- GPCR deorphanisation
- Lead optimization
Cell surface receptor assays
HTRF functionnal assays
- ERK phosphorylation assay
- cAMP cell-based assays
- cAMP membrane assys with cAMP HiRange kit
- IP-One HTRF assays
- IP-One ELISA assays
Assay Principle:
The Tag-lite internalization assay is based on a reduction of the HTRF signal. The detection reagent used is non-permeable containing the HTRF acceptors. When the receptor is at the cell surface, HTRF occur between the SNAP-Lumi4-Tb labeled GPCR and the detection reagent in the medium. When the receptor is internalized, energy transfer can no longer occurs causing a reduced HTRF signal.
In the presence of a specific agonist, the GPCR desensitization induces receptor internalization, causing the HTRF signal to plummet.
The detection reagent is universal, GPCR non-specific, allowing this method to be used for other classes of membrane receptors.
Selection of validated receptors for Tag-lite internalization assays
| Receptor family | Receptor |
| Adrenergic | Beta2 |
| Angiotensin | AT1 |
| Chemokine | CXCR4 |
| CXCR7 | |
| CCR1 | |
| CCR5 | |
| Prostanoid | EP2 |
| EP4 |
| Receptor family | Receptor |
| Cholecystokinin | CCK1 |
| CCK2 | |
| Tachykinin | NK1 |
| NK2 | |
| Vasoactive Intestinal Peptide | VPAC1 |
| Vasopressin/Oxytocin | V1A |
| V2 |
Assay in action: VPAC1 internalization assay
Internalization of VPAC1, after VIP ligand activation, was monitored quantitatively by Tag-lite internalization kinetic assay and TRF microscopy.
Tag-lite VPAC1 receptor cells were labelled with SNAP-Lumi4Tb, and plated. Detection reagent was added to the medium in large excess. A dose response was performed using VIP, a natural agonist of VPAC1 receptor, and the HTRF signal measured after 0, 10, 30, 60 and 90 min stimulation. TRF microscopic images were also shot.
A clear, strong correlation can be seen between the Tag-lite HTS internalization assay and the microscopy technique.
The Tag-lite Internalization assay service offer:
For more information or To Place an Order:
Europe and other countries
+33(0)466 796 705
