High Content Screening to Monitor G Protein-Coupled Receptor Internalisation

摘要: G protein-coupled receptors (GPCRs) fulfil a broad diversity of physiological functions in areas such as neurotransmission, respiration, cardiovascular action, pain and more. Consequently, they are considered the most successful group therapeutic targets on pharmaceutical market, search for compounds that interfere with GPCR function specific selective way is major focus industry. High Content Screening (HCS), combination fluorescence microscopic imaging automated image analysis, has become frequently employed tool to study test compound effects cellular disease modelling systems. One functionally analyse effect GPCRs by HCS relies broadly observed phenomenon desensitisation. Agonist stimulation leads their intracellular phosphorylation subsequent internalisation, resulting termination receptor signalling seclusion from further extracellular stimulation. Complementary other functional drug discovery assays, internalisation assays enable desensitisation-focussed pharmacological analysis compounds.