GPCR Internalization

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The most advanced application, published in the Journal of Biomolecular Screening, is a homogeneous assay for GPCR internalization. By creating FAP fusions w/GPCRs and using cell impermeant dyes, cell-surface GPCRs can be easily quantified. Adding dye after agonist shows a dose-dependent and time-dependant decrease in fluorescence.

An advantage to the FAPs is that they provide a direct fluorescent tagging of the GPCR, so using permeant and impermeant dyes you can easily reveal the spatial distribution of the receptor using the same assay as creates the homogeneous signals shown above.

is developing a catalog of GPRC internalization assays. Contact them with inquiries.