GPCR De-orphanization
In addition to our screening and profiling services, DiscoveRx also offers a unique method in which to deorphanize GPCRs. As a universal G protein-independent assay that generates a receptor specific signal, the PathHunter β-Arrestin platform is ideal for de-orphanization campaigns. Our Orphan Receptor Panel has been successfully used for the identification of novel ligand and receptor pairings. With 76 ready-to-assay oGPCR cell lines, we can deliver full panel screening data in less than 4 weeks
Our De-orphanization Service offers
•Access to 76 ready-to-assay oGPCR cell lines
•Universal G-protein independent assay
•Proven ability to identify receptor: ligand pairs*
•Fast turnaround for full panel screens
(click on figure to enlarge)
Figure 1. PathHunter GPR35 Orphan GPCR Cell Line
(A) EAstern blot showing a band at ~34 kDa in Lane 3, the appropriate size for GPR35 demonstrating that we have
expression and post-translational modification of the receptor.
(B) Dose response curve for Zaprinast,
a "surrogate" ligand for GPR35 showing the expected response to the agonist.
(click on figure to enlarge)
Figure 2. Example hit identified in a profile of 275 compounds against a subset of the oGPCR panel demonstrating the utility of
PathHunter technology in de-orphanization campaigns.
Available Collaterals
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Orphan Receptor Panel
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