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BRET2 Assay using the FDSS/µCELL: Monitoring cell Surface-Receptor Internalization

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BRET2 Assay using the FDSS/µCELL: Monitoring cell Surface-Receptor Internalization

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After the publication of application note No. 23 describing BRET1 technology and based on a study published in 2011, Pierre Fabre Research Institute recently implemented the more sensitive BRET2 technology to the FDSS/µCell system for monitoring the internalization of the human dopaminergic D2s- receptor (short splice form), a prototypic G protein-coupled receptor (GPCR). Internalization and endocytosis of GPCRs are dynamic processes that prevent from acute overstimulation. The inner cell-surface-located Kras GTPase protein can be used as a general inert marker for monitoring the presence or absence of a receptor at the plasma membrane. Upon receptor activation triggering its internalization, we could monitor distance changes between the receptor and the GTPase protein, and observed a BRET decrease between the receptor and the Kras.

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