PathHunter™ β-Arrestin Orphan GPCR Assays
Universal, G-Protein Independent Technology Ideal for GPCR De-Orphanization
In spite of the proven track record of GPCRs as druggable targets, approximately
100 non-odorant GPCRs remain to have their cognate ligands identified and are
therefore referred to as orphan GPCRs. PathHunter™ β-Arrestin Orphan GPCR assays
provide the ideal screening approach to orphan GPCR drug discovery. GPCR activation
is detected using a single addition, HTS friendly, chemiluminescent reagent and is
analyzed without waiting for reporter gene activity or without knowing the second
messenger signaling of the target receptor. Only activation of the tagged GPCR
yields signal, providing a system unaffected by endogenous receptor and virtually
eliminating false positive hits associated with other assays.
Product Features
•Over 90 PathHunter™ β-Arrestin orphan GPCR assays available
•Universal, non-G-protein mediated signaling pathway
•Simple, single addition homogeneous assay ideal for HTS
•Demonstrated success in identifying receptor:ligand pair
•Ideal for surrogate ligand discovery, de-orphanization and profiling
For instrument compatibility, please click here.
Easily Deorphanize any Orphan GPCR
(click on figure to enlarge)
Figure 1. Easily deorphanize any orphan GPCR using validated cell lines
(A) Expression of the GPR35 oGPCR receptor was confirmed by EAstern blot, as shown by the
presence of a 34 KD band (lane 3). (B) Dose response curve for Zaprinast, a “surrogate” ligand
for GPR35 showing a robust response to agonist.
Don't see your target?
Click here to explore our Custom Assay Development possibilities.
Don't want to do cell culture?
New! Bulk cell options are available with the purchase of any PathHunter clone.
Package sizes range from 100 million to 3 billion cells. Bulk cells are functional
tested for optimal assay performance and are confirmed to be Mycoplasma-free.
Combine frozen, assay-ready bulk cells with PathHunter-Approved Cell Plating
Reagent and Control Ligand to expedite your screening campaigns and ensure
optimal and reproducible results every time.
Click here for a quote.
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