Receptor internalization after agonist binding and signal transduction is a feature of many GPCR, leading to degradation and long-term desensitization, or recycling to the cell surface for the next round of stimulation. This important phenomenon needs to be addressed in Drug Discovery programs as it can lead either to therapeutic or adverse effects. Moreover, as this event is independent of the exact nature of G-protein coupling, it is particularly suited to study orphan receptors for which there is little-to-no information about their physiological signaling cascades.
Using the TagLite® technology, Euroscreen has now added a brand new line of internalization assays to its already extensive GPCR testing catalogue. Targets currently available include GPR84, GIP, human and mouse GLP-1, GPR17 and GPR55. New assays will be added regularly but we can also perform custom assay development for a soft budget and with a fast turn-around-time.