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KMID : 0606920110190010001
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Biomolecules & Therapeutics
2011 Volume.19 No. 1 p.1 ~ p.8
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Platform Technologies for Research on the G Protein Coupled Receptor: Applications to Drug Discovery Research
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Lee Sung-Hou
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Abstract
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G-protein coupled receptors (GPCRs) constitute an important class of drug targets and are involved in every aspect of human physiology including sleep regulation, blood pressure, mood, food intake, perception of pain, control of cancer growth, and immune response. Radiometric assays have been the classic method used during the search for potential therapeutics acting at various GPCRs for most GPCR-based drug discovery research programs. An increasing number of diverse small molecules, together with novel GPCR targets identifi ed from genomics efforts, necessitates the use of high-throughput assays with a good sensitivity and specifi city. Currently, a wide array of high-throughput tools for research on GPCRs is available and can be used to study receptor-ligand interaction, receptor driven functional response, receptor-receptor interaction,and receptor internalization. Many of the assay technologies are based on luminescence or fl uorescence and can be easily applied in cell based models to reduce gaps between in vitro and in vivo studies for drug discovery processes. Especially, cell based models for GPCR can be effi ciently employed to deconvolute the integrated information concerning the ligand-receptor-function axis obtained from labelfree detection technology. This review covers various platform technologies used for the research of GPCRs, concentrating on the principal, non-radiometric homogeneous assay technologies. As current technology is rapidly advancing, the combination of probe chemistry, optical instruments, and GPCR biology will provide us with many new technologies to apply in the future.
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KEYWORD
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G protein coupled receptor, Calcium mobilization, Drug discovery, Receptor interaction, Time resolved fluorescence, Luminescence
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