Towards the miniaturization of GPCR-based live-cell screening assays

G protein-coupled receptors (GPCRs) play a key role in many physiological or disease-related processes and for this reason are favorite targets of the pharmaceutical industry. Although ∼30% of marketed drugs target GPCRs, their potential remains largely untapped. The discovery of new leads calls for...

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Veröffentlicht in:	Trends in biotechnology (Regular ed.) 2012-11, Vol.30 (11), p.566-574
Hauptverfasser:	Martins, Sofia A.M, Trabuco, João R.C, Monteiro, Gabriel A, Chu, Virginia, Conde, João P, Prazeres, D. Miguel F
Format:	Artikel
Sprache:	eng
Schlagworte:	Assaying automation Automation - methods Biological and medical sciences Biosensing Techniques - methods Biosensors Biotechnology cell microarrays drug discovery Drug Evaluation, Preclinical - methods drugs Enzymes Equilibrium Fundamental and applied biological sciences. Psychology G protein-coupled receptors Gene expression Health. Pharmaceutical industry high-throughput screening High-Throughput Screening Assays - methods Industrial applications and implications. Economical aspects Internal Medicine Kinases Libraries Ligands Microarray Analysis - methods microarray technology Microfluidics Microfluidics - methods Miniaturization Miniaturization - methods Miscellaneous Pharmaceutical industry Platforms Proteins Receptors Receptors, Opioid - metabolism Screening Signal transduction Technological change Trends
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Beschreibung
Zusammenfassung:	G protein-coupled receptors (GPCRs) play a key role in many physiological or disease-related processes and for this reason are favorite targets of the pharmaceutical industry. Although ∼30% of marketed drugs target GPCRs, their potential remains largely untapped. The discovery of new leads calls for the screening of thousands of compounds with high-throughput cell-based assays. Although microtiter plate-based high-throughput screening platforms are well established, microarray and microfluidic technologies hold potential for miniaturization, automation, and biosensor integration that may well redefine the format of GPCR screening assays. This paper reviews the latest research efforts directed to bringing microarray and microfluidic technologies into the realm of GPCR-based, live-cell screening assays.
ISSN:	0167-7799 1879-3096
DOI:	10.1016/j.tibtech.2012.07.004