NanoBRET to probe ligand-receptor and receptor-receptor interactions in living cells

This thesis describes a novel technique known as NanoBRET to monitor direct binding of a drug to its cognate receptor in living mice. It also describes the application of this technology to investigate interactions between two major transmembrane receptor proteins, namely Vascular endothelial receptor 2 (VEGFR2) and β2-adrenoceptor. The vascular endothelial growth factor A (VEGF-A) mediates cancer angiogenesis via its receptor VEGFR2. Here we demonstrate for the first time that VEGFR2 interacts functionally with β2-adrenoceptor. Taken together, our data suggest that protein-protein interactions between VEGFR2, the β2-adrenoceptor and their cognate signalling proteins may provide novel drug targets for cancer angiogenesis.