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This version was published on December 1, 2005
Journal of Biomolecular Screening, Vol. 10, No. 8, 765-779 (2005)
DOI: 10.1177/1087057105280517

G-Protein-Coupled Receptors in Drug Discovery: Nanosizing Using Cell-Free Technologies and Molecular Biology Approaches

Wayne R. Leifert

CSIRO Molecular and Health Technologies, Adelaide, SA, Australia

Amanda L. Aloia

CSIRO Molecular and Health Technologies, Adelaide, SA, Australia; School of Biological Sciences

Olgatina Bucco

CSIRO Molecular and Health Technologies, Adelaide, SA, Australia; Department of Medical Biochemistry, School of Medicine, Flinders University, Bedford Park, SA, Australia

Richard V. Glatz

Edward J. McMurchie

CSIRO Molecular and Health Technologies, Adelaide, SA, Australia

Signal transduction by G-protein-coupled receptors (GPCRs) underpins a multitude of physiological processes. Ligand recognition by the receptor leads to activation of a genericmolecular switch involving heterotrimeric G-proteins and guanine nucleotides. Signal transduction has been studied extensively with both cell-based systems and assays comprising isolated signaling components. Interest and commercial investment in GPCRs in areas such as drug targets, orphan receptors, highthroughput screening, biosensors, and so on will focus greater attention on assay development to allow for miniaturization, ultra-high throughput and, eventually, microarray/biochip assay formats. Although cell-based assays are adequate for many GPCRs, it is likely that these formatswill limit the development of higher density GPCRassay platforms mandatory for other applications. Stable, robust, cell-free signaling assemblies comprising receptor and appropriate molecular switching components will form the basis of future GPCR assay platforms adaptable for such applications as microarrays. The authors review current cell-free GPCR assay technologies and molecular biological approaches for construction of novel, functional GPCR assays.

Key Words: GPCR • G-proteins • HTS • cell-free • nanotechnology


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