title: Towards the miniaturization of GPCR-based live-cell screening assays.
abstract: 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.
authors.affiliation: IBB-Institute for Biotechnology and Bioengineering, Centre for Biological and Chemical Engineering, Department of Bioengineering, Instituto Superior Técnico, Technical University of Lisbon, 1049-001 Lisbon, Portugal.
authors.forename: Sofia A M
authors.initials: SA
authors.lastname: Martins
authors.forename: João R C
authors.initials: JR
authors.lastname: Trabuco
authors.forename: Gabriel A
authors.initials: GA
authors.lastname: Monteiro
authors.forename: Virginia
authors.initials: V
authors.lastname: Chu
authors.forename: João P
authors.initials: JP
authors.lastname: Conde
authors.forename: D Miguel F
authors.initials: DM
authors.lastname: Prazeres
mesh_terms: D001331:Automation / Q000379:methods; D015374:Biosensing Techniques / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D057166:High-Throughput Screening Assays / Q000379:methods; D046228:Microarray Analysis / Q000379:methods; D044085:Microfluidics / Q000379:methods; D008904:Miniaturization / Q000379:methods*; D011957:Receptors, Opioid / Q000378:metabolism*
chemical_list: C091041:G protein-coupled receptor C3; D011957:Receptors, Opioid