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 different classes of compounds including agonist, antagonist and inverse agonist, 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:
Tag-lite internalization assay is based on the drop-off of the high dynamic FRET occurring between the SNAP-Lumi4Tb labeled at the GPCR N-term position and the universal non specific GPCR detection reagent added to the medium.
In the presence of a specific agonist, the GPCR desensitization induces receptor internalization, causing the dynamic FRET to plummet.
The detection reagent is universal and GPCR non-specific, allowing this method to be used for other internalization cell 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 | |
| Lysophospholipid | S1P1 |
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 offers:
Tag-lite internalization is offered to you as a multistep service:
