| abstract |
Bioluminescence resonance energy transfer (BRET) biosensors for assessing the intracellular localization, internalization and transport to cellular compartments of proteins such as receptors and other biomolecules such as second messengers are disclosed. These biosensors, which rely on the concentration/density of BRET donors and acceptors in cellular compartments rather than specific protein-protein interactions, use the Renilla GFP/Luc BRET pair, which allows robust and reproducible monitoring of protein trafficking/localization, It has a sensitivity compatible with high-throughput screening (HTS). Also disclosed are the uses of these biosensors for various applications including assessment/monitoring of protein endocytosis, recycling and intracellular trafficking, receptor maturation/rescue by drug chaperones, various endocytosis/exocytosis process, activation/inhibition, and biomolecule concentration/density in different cellular compartments. |