Determination of ligand-induced GPCR function by luminescence-based assays ...

The human genome encodes approximately 800 G protein-coupled receptors (GPCRs), which are involved in various physiological regulation processes. This makes them valuable targets for the treatment of pain, cardiovascular, pulmonary, neurodegenerative, neurological, and gastrointestinal diseases. Approximately 34 % of FDA-approved drugs target 108 different GPCRs highlighting the potential of addressing this class of receptors. In modern drug development, the design of ligands with highly specific signaling profiles including receptor subtype selectivity, functional selectivity between different signaling pathways, and location bias is a highly desirable but often challenging objective. The aim of this thesis was the biological investigation of novel ligands from our laboratory that target the β1/β2 adrenergic receptors, the μ opioid receptor, and the orexin-1 receptor. Suitable biological in vitro assay systems were successfully established and optimized for each of the specific questions addressed to ...