GPCR dimer assays with Tag-lite® technology

G-Protein Coupled Receptors (GPCRs) are common drug targets.

Previously, most studies were based on the monomeric model, but this perception of GPCRs is now evolving towards homodimeric , heterodimeric and oligomeric models. To facilitate research into GPCR dimers, CisBio Bioassays has applied the Tag-lite® technology to GPCR interaction assays. Based on HTRF® technology, plasmids have been designed to express either the SNAP-Tag or the CLIP-Tag at the N-terminus of GPCRs, allowing the labelling of two GPCRs (identical or different) with two different fluorescent probes.
Through the TR-FRET signal, interaction between two GPCRs can be investigated.

Applications:

• Receptor deorphanization: a GPCR could be deorphanized by a drug through the characterization of a GPCR heterodimeric complex.
• New GPCR targets: to identify heterodimer specific drugs or bivalent drugs on homodimers.

Tag-lite plasmids are available for many targets:

Adenosine A1, A3
Adrenergic Alpha1A, Beta2
Anaphylatoxin C5a
Angiotensin AT1, AT2
Bombesin BB2, BRS3
Bradykinin B1, B2
Cannabinoid CB1
Chemokine CCR1, CCR2, CCR3, CCR4, CCR5, CCR6, CX3CR1, CXCR1, CXCR2, CXCR3, CXCR4, CXCR5, CXCR6, CXCR7
Cholecystokinin CCK1, CCK2
Corticotropin-Releasing Factor CRF1
Dopamine D1, D2, D2L
Endothelin ETA, ETB
Galanin GAL2
Ghrelin GHSR1, A
Glucagon GIPR, GLP1, GLP2
Growth-releasing hormone GHRHR
Histamine H1, H2
Leukotriene/lipoxin CysLT1, CysLT2
Lysophosphatidic acid receptor EDG4
Melanocortin MC2, MC3, MC4, MC5
Metabotropic glutamate mGluR5
Muscarinic M3
Neuropeptide FF NPFFR1
Neuropeptide Y Y1, Y2, Y5
Neurotensin NTS1
N-formylpeptide FPR2
Opioid Delta opioid, Kappa opioid, Mu opioid
Orexin OX1, OX2
Parathyroid PTH1
Prolactin-releasing peptide PRRP
Serotonin 5HT1A, 5HT2A, 5HT2B, 5HT2C
Tachykinin NK1, NK2
Vasoactive Intestinal Peptide PAC1, VPAC1, VPAC2
Vasopressin/Oxytocin V1a, V2

Please contact CisBio for more information on other GPCRs.