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PathHunter® GPCR Internalization Detection
Upon activation, most cell surface receptors are internalized in a process called
endocytosis. Endocytosis is a fundamental component of GPCR
biology that regulates the amount of cell-surface receptors, helps to transduce signals from
the receptor as well as controls the recycling or degradation of the receptors
themselves. Regulated internalization of receptors from the cell surface modulates
cell sensitivity to specific ligands.
Download the user manual (Activated) 
Product Features
Over 80 functional whole cell GPCR assays available
Pre-validated, stable cell lines expressing the GPCR of interest
Direct measure of internalized GPCRs targeted to early endosomes
Quantitative gain-of-signal assay
No antibodies, imaging or radioactivity
HTS-friendly format
Two Novel GPCR Internalization Systems
DiscoveRx's team of experienced GPCR biologists has developed 2 novel GPCR
endocytosis assays to enable your drug discovery programs. Both assays are
non-imaging, non-antibody based chemiluminescent detection platforms that
provide a direct and quantitative measurement of internalized GPCRs in live cells.
PathHunter® Activated GPCR Internalization Assays detect Arrestin-mediated
GPCR internalization. In this system, the small enzyme fragment of β-galactosidase
called ProLink™ (PK) is localized to intracellular endosomes and the larger
complementing enzyme fragment termed Enzyme Acceptor or EA is fused to
β-Arrestin. Stimulation of the receptor results in Arrestin binding to the activated
GPCR, internalization of the receptor and trafficking to cellular endosomes. This
action forces complementation of the two enzyme fragments, resulting in an increase
in enzyme activity that is easily measured using PathHunter® Detection Reagents.
Click on figure to enlarge
PathHunter® Total GPCR Internalization System, the large portion of β-galactosidase called Enzyme Acceptor or EA is localized exclusively to intracellular endosomes and PK is fused to the GPCR of interest. GPCR activation results in internalization of the receptor and trafficking to endosomes. This action forces complementation of the two enzyme fragments, resulting in an increase in enzyme activity that is easily measured using PathHunter® Detection Reagents.
Download the user manual (Total)
Click on figure to enlarge
New! Assay Ready eXpress Format
Available Literature
Click here to view what we have available!
Want to learn more?
Download
a 30 minute tutorial on our PathHunter Internalization assays.
Download the slides.
Don't see your target?
Click here to explore our Custom Assay Development possibilities.
New! PathHunter® Certified Cell Plating Reagents & Control Ligands
For a complete list of all GPCR targets, click here.
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