PathHunter™ GPCR Endocytosis 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.

Two Novel Endocytosis Assays

DiscoveRx's team of experienced GPCR biologists has developed 2 novel GPCR
endocytosis assays to enable your drug discovery programs. Both assays were
designed using the low-affinity enzyme complementation technology which
relies on protein proximity to yield complementation of two partial fragments of
β-galactosidase and utilize chemiluminescence as the assay readout.

PathHunter™ Activated GPCR Internalization Assays provide a quantitative measurement of internalized GPCR protein localized to the endocytic compartment and let you monitor the cellular fate of unlabeled, arrestin-bound GPCRs in live cells. Unlike other imaging or antibody-based internalization technologies, PathHunter assays are simple, non-radioactive chemiluminescent assays that are amerable to high throughput screening.

               (click on figure to enlarge)                             (click on figure to enlarge)

Available Collaterals

click here to view what we have available!

PathHunter™ Total GPCR Endocytosis Assay provides a quantitative measurement of total GPCR protein whether it is localized to the cell surface or internalized into endosomes.

In this system, one enzyme fragment is localized exclusively to the surface of
cellular endosomes and the complementing enzyme fragment is fused to the GPCR of interest. Stimulation of the target receptor results in internalization of the receptor and trafficking to cellular endosomes. This action forces the complementation of
the two enzyme fragments, resulting in an increase in enzyme activity that is easily measured using chemiluminescent PathHunter™ Detection Reagents.

               (click on figure to enlarge)                             (click on figure to enlarge)

Don't see your target?

Click here to explore our Custom Assay Development possibilities.

For a complete list of all GPCR targets, click here.

 

Copyright ©2009, DiscoveRx Corporation. TERMS AND CONDITIONS