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The development of label-free cellular assays for drug discovery

Pages 1285-1298 | Published online: 01 Dec 2011

Bibliography

  • Swinney DC, Anthony J. How were new medicines discovered? Nat Rev Drug Discov 2011;10:507-19
  • Kenakin T. Cellular assays as portals to seven-transmembrane receptor-based drug discovery. Nat Rev Drug Discov 2009;8:617-26
  • Inglese J, Johnson RL, Simeonov A, High-throughput screening assays for the identification of chemical probes. Nat Chem Biol 2007;3:466-79
  • Gleeson M, Hersey A, Montanari D, Overington J. Probing the links between in vitro potency, ADMET and physicochemical parameters. Nat Rev Drug Discov 2011;10:197-208
  • Butcher E. Can cell systems biology rescue drug discovery? Nat Rev Drug Discov 2005;4:461-7
  • Kepp O, Galluzzi L, Lipinski M, Cell death assays for drug discovery. Nat Rev Drug Discov 2011;10:221-37
  • Navratilova I, Besnard J, Hopkins AL. Screening for GPCR ligands using surface plasmon resonance. ACS Med Chem Lett 2011;2:549-54
  • Fang Y. Label-free cell-based assays with optical biosensors in drug discovery. Assay Drug Dev Technol 2006;4:583-95
  • McGuinness R. Impedance-based cellular assay technologies: recent advances, future promise. Curr Opin Pharmacol 2007;7:535-40
  • Fang Y. Label-free receptor assays. Drug Discov Today Technol 2010;7:e5-e11
  • Scott CW, Peters MF. Label-free whole-cell assays: expanding the scope of GPCR screening. Drug Discov Today 2010;15:704-16
  • Giaever I, Keese CR. Monitoring fibroblast behavior in tissue culture with an applied electric field. Proc Natl Acad Sci USA 1984;81:3761-4
  • Giaever I, Keese CR. A morphological biosensor for mammalian cells. Nature 1993;366:591-2
  • Fang Y, Ferrie AM, Li G. Probing cytoskeleton modulation by optical biosensors. FEBS Lett 2005;579:4175-80
  • Fang Y, Ferrie AM, Fontaine NH, Yuen PK. Characteristics of dynamic mass redistribution of EGF receptor signaling in living cells measured with label free optical biosensors. Anal Chem 2005;77:5720-5
  • Fang Y, Li G, Peng J. Optical biosensor provides insights for bradykinin B2 receptor signaling in A431 cells. FEBS Lett 2005;579:6365-74
  • Corning Epic® system. Available from: http://www.corning.com/lifesciences/epic/en/index.aspx
  • Fang Y. Non-invasive optical biosensor for probing cell signaling. Sensors 2007;7:2316-29
  • PerkinElmer EnSpire™ reader. Available from: http://www.perkinelmer.com/Catalog/Family/ID/EnSpire
  • SRU BioSystems BIND™ system. Available from: http://www.srubiosystems.com
  • Shamah SM, Cunningham BT. Label-free cell-based assays using photonic crystal optical biosensors. Analyst 2011;136:1090-102
  • Applied BioPhysics ECIS™ system. Available from: http://www.biophysics.com
  • Roche/Acea Biosciences xCELLigence™ system. Available from: www.roche-applied-science.com
  • Yu N, Atienza JM, Bernard J, Real-time monitoring of morphological changes in living cells by electronic cell sensor arrays: an approach to study G protein-coupled receptors. Anal Chem 2006;78:35-43
  • Molecular Devices CellKey™ system. Available from: http://www.cellkey.com
  • Ciambrone GJ, Liu VF, Lin DC, Cellular dielectric spectroscopy: a powerful new approach to label-free cellular analysis. J Biomol Screen 2004;9:467-80
  • Ramsden JJ, Horvath R. Optical biosensors for cell adhesion. J Recept Signal Transduct 2009;29:211-23
  • Wegener J, Keese CR, Giaever I. Electric cell-substrate impedance sensing (ECIS) as a noninvasive means to monitor the kinetics of cell spreading to artificial surfaces. Exp Cell Res 2000;259:158-66
  • Tiruppathi C, Malik AB, del Vecchio PJ, Electrical method for detection of endothelial cell shape change in real time: Assessment of endothelial barrier function. Proc Natl Acad Sci USA 1992;89:7919-23
  • McLaughlin JN, Shen L, Holinstat M, Functional selectivity of G protein signaling by agonist peptides and thrombin for the protease-activated receptor-1. J Biol Chem 2005;280:25048-59
  • Fang Y. Label-free biosensors for cell biology. Int J Electrochem. 2011;2011:e460850
  • Xing JZ, Zhu L, Jackson JA, Dynamic monitoring of cytotoxicity on microelectronic sensors. Chem Res Toxicol 2005;8:154-61
  • Opp D, Wafula B, Lim J, Use of electric cell-substrate impedance sensing to assess in vitro cytotoxicity. Biosens Bioelectron 2009;24:2625-9
  • Kataoka N, Iwaki K, Hashimoto K, Measurements of endothelial cell-to-cell and cell-to-substrate gaps and micromechanical properties of endothelial cells during monocyte adhesion. Proc Natl Acad Sci USA 2002;99:15638-43
  • Glamann J, Hansen AJ. Dynamic detection of natural killer cell-mediated cytotoxicity and cell adhesion by electrical impedance measurements. Assay Drug Dev Technol 2006;4:555-63
  • Bagnaninchi PO, Drummond N. Real-time label-free monitoring of adipose-derived stem cell differentiation with electric cell-substrate impedance sensing. Proc Natl Acad Sci USA 2011;108:6462-7
  • Spiering D, Schmolke M, Ohnesorge N, MEK5/ERK5 signaling modulates endothelial cell migration and focal contact turnover. J Biol Chem 2009;284:24972-80
  • Wang L, Zhu J, Deng C, An automatic and quantitative on-chip cell migration assay using self-assembled monolayers combined with real-time cellular impedance sensing. Lab Chip 2008;8:872-8
  • Rutkove SB. Electrical impedance for assessing muscle. J Biomol Screen 2011;16:798-9
  • Rakhilin S, Turner G, Katz M, Electrical impedance as a novel biomarker of myotube atrophy and hypertrophy. J Biomol Screen 2011;16:565-74
  • Abassi YA, Xi B, Li N, Dynamic monitoring of beating periodicity of stem cell derived cardiomyocytes as a predictive tool for preclinical safety assessment. Br J Pharmacol 2011; published online 12 Aug, 2011; doi: 10.1111/j.1476-5381.2011.01623.x.
  • McCoy MH, Wang E. Use of electric cell-substrate impedance sensing as a tool for quantifying cytopathic effect in influenza a virus infected MDCK cells in real-time. J Virol Methods 2005;130:157-61
  • Owens RM, Wang C, You JA, Real-time quantitation of viral replication and inhibitor potency using a label-free optical biosensor. J Recept Signal Transduct 2009;29:195-201
  • Fang Y, Li G, Ferrie AM. Non-invasive optical biosensor for assaying endogenous G protein-coupled receptors in adherent cells. J Pharamcol Toxicol Methods 2007;55:314-22
  • Peters MF, Vaillancourt F, Heroux M, Comparing label-free biosensors for pharmacological screening with cell-based functional assays. Assay Drug Dev Technol 2010;8:219-27
  • Fang Y, Ferrie AM, Tran E. Resonant waveguide grating biosensor for whole cell GPCR assays. Methods Mol Biol 2009;552:239-52
  • Atienza JM, Yu N, Wang X, Label-free and real-time cell-based kinase assay for screening selective and potent receptor tyrosine kinase inhibitors using microelectronic sensor array. J Biomol Screen 2006;11:634-43
  • Du Y, Li Z, Li L, Distinct growth factor-induced dynamic mass redistribution (DMR) profiles for monitoring oncogenic signaling pathways in various cancer cells. J Recept Signal Transduct 2009;29:182-94
  • Panke O, Weigel W, Schmidt S, A cell-based impedance assay for monitoring transient receptor potential (TRP) ion channel activity. Biosens Bioelectron 2011;26:2376-82
  • Fleming MR, Kaczmarek LK. Use of optical biosensors to detect modulation of Slack potassium channels by G protein-coupled receptors. J Recept Signal Transduct 2009;29:173-81
  • Abassi YA, Jackson JA, Zhu J, Label-free, real-time monitoring of IgE-mediated mast cell activation on microelectronic cell sensor arrays. J Immunol Methods 2004;292:195-205
  • Tanaka M, Hiragun T, Tsutsui T, Surface plasmon resonance biosensor detects the downstream events of active PKCbeta in antigen-stimulated mast cells. Biosens Bioelectron 2008;23:1652-8
  • Ferrie AM, Wu Q, Fang Y. Resonant waveguide grating imager for live cell sensing. Appl Phys Lett 2010;97:223704
  • Coller HA, Sang L, Roberts JM. A new description of cellular quiescence. PLoS Biol 2006;4:e83
  • Deng H, Hu H, Fang Y. Tyrphostin analogs are GPR35 agonists. FEBS Lett 2011;585:1957-62
  • Sun Y, Huang J, Xiang Y, Dosage-dependent switch from G protein-coupled to G protein-independent signaling by a GPCR. EMBO J 2007;26:53-64
  • Fang Y, Ferrie AM. Label-free optical biosensor for ligand-directed functional selectivity of acting on beta2 adrenoceptor in living cells. FEBS Lett 2008;582:558-64
  • Carter AA, Hill SJ. Characterization of isoprenaline- and salmeterol-stimulated interactions between beta2-adrenergic receptors and beta-arrestin 2 using beta-galactosidase complementation in C2C12 cells. J Pharmacol Exp Ther 2005;315:839-48
  • Hern JA, Baig AH, Mashanov GI, Formation and dissociation of M1 muscarinic receptor dimers seen by total internal reflection fluorescence imaging of single molecules. Proc Natl Acad Sci USA 2010;107:2693-8
  • Metz JT, Hajduk PJ. Rational approaches to targeted polypharmacology: creating and navigating protein-ligand interaction networks. Curr Opin Chem Biol 2010;14:498-504
  • Ferrie AM, Sun H, Fang Y. Label-free integrative pharmacology on-target of drugs at the beta2-adrenergic receptor. Sci Rep 2011;1:33
  • Azzi M, Charest PG, Angers S, Pineyro G. beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors. Proc Natl Acad Sci USA 2003;100:11406-11
  • Wisler JW, DeWire SM, Whalen EJ, A unique mechanism of beta-blocker action: Carvedilol stimulates beta-arrestin signaling. Proc Natl Acad Sci USA 2007;104:16657-62
  • Mailman RB. Ligand-selective signaling and high content for GPCR drugs. Trends Pharmacol Sci 2007(12):390-6
  • Galandrin S, Oligny-Longpre G, Bouvier M. The evasive nature of drug efficacy: implications for drug discovery. Trends Pharmacol Sci 2007;8:423-30
  • Kenakin T. New concepts in drug discovery: collateral efficacy and permissive antagonism. Nat Rev Drug Discov 2005;4:919-27
  • Kenakin TP, Morgan PH. The theoretical effects of single and multiple transducer receptor coupling proteins on estimates of the relative potency of agonists. Mol Pharmacol 1989;35:214-22
  • Swaminath G, Xiang Y, Lee TW, Sequential binding of agonists to the beta2 adrenoceptor: kinetic evidence for intermediate conformational states. J Biol Chem 2004;279:686-91
  • Bokoch MP, Zou Y, Rasmussen SGF, Ligand-specific regulation of the extracellular surface of a G protein coupled receptor. Nature 2010;463:108-12
  • Deupi X, Kobilka BK. Energy landscapes as a tool to integrate GPCR structure, dynamics, and function. Physiology 2010;25:293-303
  • Kinzer-Ursem TL, Linderman JJ. Both ligand- and cell-specific parameters control ligand agonism in a kinetic model of G protein-coupled receptor signaling. PLoS Comput Biol 2007;3:e6
  • Kenakin T, Miller LJ. Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol Rev 2010;62:265-304
  • Hermans E. Biochemical and pharmacological control of the multiplicity of coupling at G-protein-coupled receptors. Pharmacol Ther 2003;99:25-44
  • Peters MF, Scott CW. Evaluating cellular impedance assays for detection of GPCR pleiotropic signaling and functional selectivity. J Biomol Screen 2009;14:246-55
  • Schroder R, Janssen N, Schmidt J, Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements. Nat Biotechnol 2010;28:943-9
  • Fang Y. Probing cancer signaling with resonant waveguide grating biosensors. Exp Opin Drug Discov 2010;5:1237-48
  • Tran E, Sun H, Fang Y. Dynamic mass redistribution assays decode surface influence on signaling of endogenous purinergic P2Y receptors. Assays Drug Dev Technol 2011; published online 8 November, 2011; doi: 10.1089/adt.2011.0392
  • Fang Y, Frutos AG, Verklereen R. Label-free cell assays for GPCR screening. Comb Chem High Throughput Screen 2008;11:357-69
  • Giuliano KA, Johnston PA, Gough A, Taylor DL. Systems cell biology based on high-content screening. Methods Enzymol 2006;414:601-19
  • Fang Y, Ferrie AM, Fontaine NH, Resonant waveguide grating biosensor for living cell sensing. Biophys J 2006;91:1925-40
  • Kholodenko BN. Four-dimensional organization of protein kinase signaling cascades: the roles of diffusion, endocytosis and molecular motors. J Exp Biol 2003;206:2073-82
  • Aldridge BB, Burke JM, Lauffenburger DA, Sorger PK. Physicochemical modelling of cell signalling pathways. Nat Cell Biol 2006;8:1195-203
  • Schnapp BJ. Trafficking of signaling modules by kinesin motors. J Cell Sci 2003;116:2125-35
  • Gangulya S, Saxenaa R, Chattopadhyay A. Reorganization of the actin cytoskeleton upon G-protein coupled receptor signaling. Biochim Biophys Acta 2011;1808:1921-9
  • Beuthan J, Minet O, Helfmann J, The spatial variation of the refractive index in biological cells. Phys Med Biol 1996;41:369-82
  • Gheorghiu E, Balut C, Gheorghiu M. Dielectric behaviour of gap junction connected cells: a microscopic approach. Phys Med Biol 2002;47:341-8
  • Schroeder R, Merten N, Mathiesen JM, The C-terminal tail of CRTH2 is a key molecular determinant that constrains Galphai- and downstream-signaling cascade activation. J Biol Chem 2009;284:1324-36
  • Verrier F, An S, Ferrie AM, GPCRs regulate the assembly of a multienzyme complex for purine biosynthesis. Nat Chem Biol 2011;7:909-15
  • Kebig A, Kostenis E, Mohr K, Mohr-Andr M. An optical dynamic mass redistribution assay reveals biased signaling of dualsteric GPCR activators. J Recept Signal Transduct 2009;29:140-5
  • Eisen MB, Spellman PT, Brown PO, Botstein D. Cluster analysis and display of genome-wide expression patterns. Proc Natl Acad Sci USA 1998;95:14863-8
  • Ke N, Xi B, Ye P, Screening and identification of small molecule compounds perturbing mitosis using time-dependent cellular response profiles. Anal Chem 2010;82:6495-503
  • Fliri AF, Loging WT, Thadeio PF, Volkmann RA. Biological spectra analysis: Linking biological activity profiles to molecular structure. Proc Natl Acad Sci USA 2005;102:261-6
  • Lamb J, Crawford ED, Peck D, The connectivity map: using gene-expression signatures to connect small molecules, genes, and disease. Science 2006;313:929-35
  • Hoon S, Smith AM, Wallace IM, An integrated platform of genomic assays reveals small-molecule bioactivities. Nat Chem Biol 2008;4:498-506
  • Young DW, Bender A, Hoyt J, Integrating high-content screening and ligand-target prediction to identify mechanism of action. Nat Chem Biol 2008;4:59-68
  • Campillos M, Kuhn M, Gavin A, Drug target identification using side-effect similarity. Science 2008;321:263-6
  • Keiser MJ, Setola V, Irwin JJ, Predicting new molecular targets for known drugs. Nature 2009;462:175-81
  • Zhao S, Li S. Network-based relating pharmacological and genomic spaces for drug target identification. PLoS ONE 2010;5:e11764
  • Kenakin T. Functional selectivity and biased receptor signaling. J Pharmacol Exp Ther 2011;336:296-302
  • Galandrin S, Bouvier M. Distinct signaling profiles of beta1 and beta2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy. Mol Pharmacol 2006;70:1575-84
  • Baker JG. The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. Br J Pharmacol 2005;144:317-22
  • Baker JG. The selectivity of beta-adrenoceptor agonists at human beta1-, beta2-, beta3-adrenoceptors. Br J Pharmacol 2010;160:1048-61
  • Bigal ME, Krymchantowski AV. Emerging drugs for migraine prophylaxis and treatment. Med Gen Med 2006;8:31
  • Lam F, Gill P. Beta-agonist tocolytic therapy. Obstet Gynecol Clin North Am 2005;32:457-84
  • Paul SM, Mytelka DS, Dunwiddie CT, How to improve R&D productivity: the pharmaceutical industry's grand challenge. Nat Rev Drug Discov 2010;9:203-14
  • Pammolli F, Magazzini L, Riccaboni M. The productivity crisis in pharmaceutical R&D. Nat Rev Drug Discov 2011;10:428-38
  • Goral V, Jin Y, Sun H, Agonist-directed desensitization of the beta2-adrenergic receptor. PLoS ONE 2011;6:e19282
  • Zaytseva N, Miller W, Goral V, Microfluidic resonant waveguide grating biosensor system for whole cell sensing. Appl Phys Lett 2011;96:163703
  • Goral V, Wu Q, Sun H, Fang Y. Label-free optical biosensor with microfluidics for sensing ligand-directed functional selectivity on trafficking of thrombin receptor. FEBS Lett 2011;585:1054-60
  • Ghenim L, Kaji H, Hoshino Y, Monitoring impedance changes associated with motility and mitosis of a single cell. Lab Chip 2010;10:2546-50
  • Sandu T, Vrinceanu D, Gheorghiu E. Linear dielectric response of clustered living cells. Phys Rev E 2010;81:021913
  • Horvath R, Cottier K, Pedersen HC, Ramsden JJ. Mutlidepth screening of living cells using optical waveguide. Biosens Bioelectron 2008;24:799-804
  • Yashunsky V, Lirtsman V, Golosovsky M, Real-time monitoring of epithelial cell-cell and cell-substrate interactions by infrared surface plasmon spectroscopy. Biophys J 2010;99:4028-36

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