Transfluor Technology
Universal GPCR assay
Transfluor is an advanced, cell-based screening technology applicable to all known and orphan GPCRs. Transfluor has been successfully validated on over 90 GPCRs and works across all GPCR classes (Class I, II, III), regardless of interacting G-protein (Gs, Gi/o and Gq/11). Transfluor eliminates the need for multiple GPCR assay platforms.
The Transfluor technology monitors receptor activity by detecting movement of ß arrestin-GFP in the cell. A partial listing of GPCRs that have been shown to translocate ß arrestin-GFP is shown below.
Partial GPCR listing
| Gs |
Gi/o |
Gq/11 |
- A2a adenosine
- A2b adenosine
- ß1-adrenergic
- ß2-adrenergic
- CRF1 corticotropin releasing factor
- D1 dopamine
- D5 dopamine
- FSH follicle-stimulating hormone
- Glucagon
- LH luteinizing hormone
- PTH1 parathyroid hormone
- E2 prostaglandin
- E4 prostaglandin
- Secretin
- VIP1 vasoactive intestinal peptide
- V2 vasopressin
|
- alpha 2a-adrenergic
- alpha 2b-adrenergic
- alpha 2c-adrenergic
- A1 adenosine
- A3 adenosine
- Apelin
- C5a anaphylatoxin
- CCR5 chemokine
- CXCR1 chemokine
- CXCR2 chemokine
- CXCR4 chemokine
- D2 dopamine
- D3 dopamine
- D4 dopamine
- Edg1 endothelial diff. gene
- Edg2 endothelial diff. gene
- Edg3 endothelial diff. gene
- Edg5 endothelial diff. gene
- 5HT1A hydroxytryptamine
- delta-opioid
- mu-opioid
- MCH1 melanin conc. hormone
- M2Ach muscarinic acetylcholine
- E3 prostaglandin
- N-formyl peptide
- Neuropeptide FF
- Somatostatin
|
- alpha 1b-adrenergic
- AT1A angiotensin II
- CCK-A cholecystokinin
- CCK-B cholecystokinin
- Cytomegalovirus US28
- ETA endothelin
- GnRH (type2) gonadotropin releasing hormone
- 5HT2A hydroxytryptamine
- 5HT2C hydroxytryptamine
- m1ACh muscarinic acetylcholine
- mGluR1 metabotropic glutamate
- NK1 neurokinin
- NK3 neurokinin
- NT1 neurotensin
- Orexin-1
- Oxytocin
- PAR2 proteinase-activated
- Platelet-activating factor
- TRHR-1 thyrotropin releasing hormone
- TRHR-2 thyrotropin releasing hormone
|
Other receptor listing
- 12 Drosophila GPCRs
- Fz4 frizzled receptor
- TßRIII transforming growth factor-ß
Orphan GPCR assay
In contrast to current methods of screening GPCRs, the Transfluor technology is based on the mechanism for termination of GPCR signaling, known as receptor desensitization. This mechanism is shared by virtually all GPCRs and is activated by ligand binding. Transfluor technology requires no prior knowledge of the interacting G-protein. This important feature of the Transfluor technology makes it ideal for screening orphan GPCRs (oGPCR).
A proprietary technique to assist in validating orphan GPCR screens, called LITe™ (Ligand Independent Translocation), is an agonist-independent assay used to verify the translocation of ß arrestin-GFP in orphan GPCRs.
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