239
Views
14
CrossRef citations to date
0
Altmetric
Reviews

High-content screening for the discovery of pharmacological compounds: advantages, challenges and potential benefits of recent technological developments

, PhD (Researcher) , , PhD (Associate Professor) & , PhD (Researcher)
Pages 135-144 | Published online: 09 Jan 2010

Bibliography

  • Evans NA, Facci L, Owen DE, A beta(1-42) reduces synapse number and inhibits neurite outgrowth in primary cortical and hippocampal neurons: a quantitative analysis. J Neurosci Methods 2008;175(1):96-103
  • Viero C, Kraushaar U, Ruppenthal S, A primary culture system for sustained expression of a calcium sensor in preserved adult rat ventricular myocytes. Cell Calcium 2008;43(1):59-71
  • Prigozhina NL, Zhong L, Hunter EA, Plasma membrane assays and three-compartment image cytometry for high content screening. Assay Drug Dev Technol 2007;5(1):29-48
  • Mouchet EH, Simpson PB. High-content assays in oncology drug discovery: opportunities and challenges. IDrugs 2008;11(6):422-7
  • Bickle M. High-content screening: a new primary screening tool? IDrugs 2008;11(11):822-6
  • Fox S, Farr-Jones S, Sopchak L, High-throughput screening: update on practices and success. J Biomol Screen 2006;11(7):864-9
  • Mayr LM, Bojanic D. Novel trends in high-throughput screening. Curr Opin Pharmacol 2009;9(5):580-8
  • Stein RL. High-throughput screening in academia: the Harvard experience. J Biomol Screen 2003;8(6):615-9
  • Inglese J, Johnson RL, Simeonov A, High-throughput screening assays for the identification of chemical probes. Nat Chem Biol 2007;3(8):466-79
  • Stockwell BR. Exploring biology with small organic molecules. Nature 2004;432(7019):846-54
  • Lafanechere L. Chemogenomics and cancer chemotherapy: cell-based assays to screen for small molecules that impair microtubule dynamics. Comb Chem High Throughput Screen 2008;11(8):617-23
  • Mitchison T. Toward pharmacological genetics. Chem Biol 1994;1:3-6
  • Fonrose X, Ausseil F, Soleilhac E, Parthenolide inhibits tubulin carboxypeptidase activity. Cancer Res 2007;67(7):3371-8
  • Korn K, Krausz E. Cell-based high-content screening of small-molecule libraries. Curr Opin Chem Biol 2007;11(5):503-10
  • Yarrow JC, Feng Y, Perlman ZE, Phenotypic screening of small molecule libraries by high throughput cell imaging. Comb Chem High Throughput Screen 2003;6(4):279-86
  • Knight ZA, Shokat KM. Features of selective kinase inhibitors. Chem Biol 2005;12(6):621-37
  • Schoonen WG, Westerink WM, Horbach GJ. High-throughput screening for analysis of in vitro toxicity. EXS 2009;99:401-52
  • Giuliano KA. High-content profiling of drug-drug interactions: cellular targets involved in the modulation of microtubule drug action by the antifungal ketoconazole. J Biomol Screen 2003;8(2):125-35
  • Ross-Macdonald P, de Silva H, Guo Q, Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors. Mol Cancer Ther 2008;7(11):3490-8
  • Wermuth CG. Selective optimization of side activities: the SOSA approach. Drug Discov Today 2006;11(3-4):160-4
  • Caldwell GW, Ritchie DM, Masucci JA, The new pre-preclinical paradigm: compound optimization in early and late phase drug discovery. Curr Top Med Chem 2001;1(5):353-66
  • Guillouzo A, Guguen-Guillouzo C. Evolving concepts in liver tissue modeling and implications for in vitro toxicology. Expert Opin Drug Metab Toxicol 2008;4(10):1279-94
  • Eglen RM, Gilchrist A, Reisine T. An overview of drug screening using primary and embryonic stem cells. Comb Chem High Throughput Screen 2008;11(7):566-72
  • Chen S, Borowiak M, Fox JL, A small molecule that directs differentiation of human ESCs into the pancreatic lineage. Nat Chem Biol 2009;5(4):258-65
  • Jaksch M, Munera J, Bajpai R, Cell cycle-dependent variation of a CD133 epitope in human embryonic stem cell, colon cancer, and melanoma cell lines. Cancer Res 2008;68(19):7882-6
  • Damoiseaux R, Sherman SP, Alva JA, Integrated chemical genomics reveals modifiers of survival in human embryonic stem cells. Stem Cells 2009;27(3):533-42
  • Peterson JR, Mitchison TJ. Small molecules, big impact: a history of chemical inhibitors and the cytoskeleton. Chem Biol 2002;9(12):1275-85
  • Feng Y, Mitchison TJ, Bender A, Multi-parameter phenotypic profiling: using cellular effects to characterize small-molecule compounds. Nat Rev Drug Discov 2009;8(7):567-78
  • Mayer TU, Kapoor TM, Haggarty SJ, Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. Science 1999;286(5441):971-4
  • Stockwell BR, Haggarty SJ, Schreiber SL. High-throughput screening of small molecules in miniaturized mammalian cell-based assays involving post-translational modifications. Chem Biol 1999;6(2):71-83
  • Crews CM, Spittgerber U. Chemical genetics: exploring and controlling cellular processes with chemical probes. Trends Biochem Sci;24:317-20
  • Burdine L, Kodadek T. Target identification in chemical genetics: the (often) missing link. Chem Biol 2004;11(5):593-7
  • Peterson JR, Lokey RS, Mitchison TJ, Kirschner MW. A chemical inhibitor of N-WASP reveals a new mechanism for targeting protein interactions. Proc Natl Acad Sci USA 2001;98(19):10624-9
  • Carey KL, Westwood NJ, Mitchison TJ, Ward GE. A small-molecule approach to studying invasive mechanisms of Toxoplasma gondii. Proc Natl Acad Sci USA 2004;101(19):7433-8
  • Roberge M, Cinel B, Anderson HJ, Cell-based screen for antimitotic agents and identification of analogues of rhizoxin, eleutherobin, and paclitaxel in natural extracts. Cancer Res 2000;60(18):5052-8
  • An WF, Tolliday NJ. Introduction: cell-based assays for high-throughput screening. Methods Mol Biol 2009;486:1-12
  • Clemons PA. Complex phenotypic assays in high-throughput screening. Curr Opin Chem Biol 2004;8(3):334-8
  • Li X, Shen F, Zhang Y, Functional characterization of cell lines for high-throughput screening of human neuromedin U receptor subtype 2 specific agonists using a luciferase reporter gene assay. Eur J Pharm Biopharm 2007;67(1):284-92
  • Vassal E, Barette C, Fonrose X, Miniaturization and validation of a sensitive multiparametric cell-based assay for the concomitant detection of microtubule-destabilizing and microtubule-stabilizing agents. J Biomol Screen 2006;11(4):377-89
  • Bradley J, Gill J, Bertelli F, Development and automation of a 384-well cell fusion assay to identify inhibitors of CCR5/CD4-mediated HIV virus entry. J Biomol Screen 2004;9(6):516-24
  • Perlman ZE, Mitchison TJ, Mayer TU. High-content screening and profiling of drug activity in an automated centrosome-duplication assay. Chembiochem 2005;6(1):145-51
  • Yarrow JC, Totsukawa G, Charras GT, Mitchison TJ. Screening for cell migration inhibitors via automated microscopy reveals a Rho-kinase inhibitor. Chem Biol 2005;12(3):385-95
  • Yarrow JC, Perlman ZE, Westwood NJ, Mitchison TJ. A high-throughput cell migration assay using scratch wound healing, a comparison of image-based readout methods. BMC Biotechnol 2004;4:21
  • Gasparri F, Ciavolella A, Galvani A. Cell-cycle inhibitor profiling by high-content analysis. Adv Exp Med Biol 2007;604:137-48
  • Wilson CJ, Si Y, Thompsons CM, Identification of a small molecule that induces mitotic arrest using a simplified high-content screening assay and data analysis method. J Biomol Screen 2006;11(1):21-8
  • Castel D, Pitaval A, Debily MA, Gidrol X. Cell microarrays in drug discovery. Drug Discov Today 2006;11(13-14):616-22
  • Mitchison TJ. Small-molecule screening and profiling by using automated microscopy. Chembiochem 2005;6(1):33-9
  • Loo LH, Lin HJ, Steininger RJ III, An approach for extensibly profiling the molecular states of cellular subpopulations. Nat Methods 2009;6(10):759-65
  • Chakraborty C, Hsu CH, Wen ZH, Lin CS. Recent advances of fluorescent technologies for drug discovery and development. Curr Pharm Des 2009;15(30):3552-70
  • Wolff M, Wiedenmann J, Nienhaus GU, Novel fluorescent proteins for high-content screening. Drug Discov Today 2006;11(23-24):1054-60
  • Tsui M, Xie T, Orth JD, An intermittent live cell imaging screen for siRNA enhancers and suppressors of a kinesin-5 inhibitor. PLoS One 2009;4(10):e7339
  • Daub A, Sharma P, Finkbeiner S. High-content screening of primary neurons: ready for prime time. 0Curr Opin Neurobiol 2009;19:537-43
  • Neumann B, Held M, Liebel U, High-throughput RNAi screening by time-lapse imaging of live human cells. Nat Methods 2006;3(5):385-90
  • Zhou X, Cao X, Perlman Z, Wong ST. A computerized cellular imaging system for high content analysis in Monastrol suppressor screens. J Biomed Inform 2006;39(2):115-25
  • Zhou X, Wong ST. Informatics challenges of high-troughput microscopy. Ieee Signal Processing Magazine 2006;23:63-72
  • Carpenter AE. Image-based chemical screening. Nat Chem Biol 2007;3(8):461-5
  • Maloney KN, Fujita M, Eggert US, Actin-Aggregating Cucurbitacins from Physocarpus capitatus. J Nat Prod 2008;71:1927-9
  • Peters U, Cherian J, Kim JH, Probing cell-division phenotype space and Polo-like kinase function using small molecules. Nat Chem Biol 2006;2(11):618-26
  • Eggert US, Kiger AA, Richter C, Parallel chemical genetic and genome-wide RNAi screens identify cytokinesis inhibitors and targets. PLoS Biol 2004;2(12):e379
  • Miron M, Nadon R. Inferential literacy for experimental high-throughput biology. Trends Genet 2006;22(2):84-9
  • Malo N, Hanley JA, Cerquozzi S, Statistical practice in high-throughput screening data analysis. Nat Biotechnol 2006;24(2):167-75
  • Spencer SL, Gaudet S, Albeck JG, Non-genetic origins of cell-to-cell variability in TRAIL-induced apoptosis. Nature 2009;459(7245):428-32
  • Krutzik PO, Nolan GP. Intracellular phospho-protein staining techniques for flow cytometry: monitoring single cell signaling events. Cytometry A 2003;55(2):61-70
  • Irish JM, Hovland R, Krutzik PO, Single cell profiling of potentiated phospho-protein networks in cancer cells. Cell 2004;118(2):217-28
  • Krutzik PO, Crane JM. High-content single-cell drug screening with phosphospecific flow cytometry. Orthopedics 2008;31(10)
  • Chen CS, Mrksich M, Huang S, Micropatterned surfaces for control of cell shape, position, and function. Biotechnol Prog 1998;14(3):356-63
  • Thery M, Racine V, Piel M, Anisotropy of cell adhesive microenvironment governs cell internal organization and orientation of polarity. Proc Natl Acad Sci USA 2006;103(52):19771-6
  • Thery M, Pepin A, Dressaire E, Cell distribution of stress fibres in response to the geometry of the adhesive environment. Cell Motil Cytoskeleton 2006;63(6):341-55
  • Peris L, Thery M, Faure J, Tubulin tyrosination is a major factor affecting the recruitment of CAP-Gly proteins at microtubule plus ends. J Cell Biol 2006;174(6):839-49
  • Thery M, Jimenez-Dalmaroni A, Racine V, Experimental and theoretical study of mitotic spindle orientation. Nature 2007;447(7143):493-6
  • Kwon M, Godinho SA, Chandhok NS, Mechanisms to suppress multipolar divisions in cancer cells with extra centrosomes. Genes Dev 2008;22(16):2189-203
  • Lamb J. The Connectivity Map: a new tool for biomedical research. Nat Rev Cancer 2007;7(1):54-60
  • Lamb J, Crawford ED, Peck D, The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease. Science 2006;313(5795):1929-35
  • Zhang SD, Gant TW. A simple and robust method for connecting small-molecule drugs using gene-expression signatures. BMC Bioinformatics 2008;9:258
  • Perlman ZE, Slack MD, Feng Y, Multidimensional drug profiling by automated microscopy. Science 2004;306(5699):1194-8
  • Young DW, Bender A, Hoyt J, Integrating high-content screening and ligand-target prediction to identify mechanism of action. Nat Chem Biol 2008;4(1):59-68
  • Loo LH, Wu LF, Altschuler SJ. Image-based multivariate profiling of drug responses from single cells. Nat Methods 2007;4(5):445-53
  • Wang J, Zhou X, Bradley PL, Cellular phenotype recognition for high-content RNA interference genome-wide screening. J Biomol Screen 2008;13(1):29-39
  • Peterson RT, Link BA, Dowling JE, Schreiber SL. Small molecule developmental screens reveal the logic and timing of vertebrate development. Proc Natl Acad Sci USA 2000;97(24):12965-9
  • Giacomotto J, Pertl C, Borrel C, Evaluation of the therapeutic potential of carbonic anhydrase inhibitors in two animal models of dystrophin deficient muscular dystrophy. Hum Mol Genet 2009;18(21):4089-101
  • Kritzer JA, Hamamichi S, McCaffery JM, Rapid selection of cyclic peptides that reduce alpha-synuclein toxicity in yeast and animal models. Nat Chem Biol 2009;5(9):655-63
  • Peterson RT, Shaw SY, Peterson TA, Chemical suppression of a genetic mutation in a zebrafish model of aortic coarctation. Nat Biotechnol 2004;22(5):595-9
  • Serebriiskii I, Castello-Cros R, Lamb A, Fibroblast-derived 3D matrix differentially regulates the growth and drug-responsiveness of human cancer cells. Matrix Biol 2008;27(6):573-85
  • Friedrich J, Seidel C, Ebner R, Kunz-Schughart LA. Spheroid-based drug screen: considerations and practical approach. Nat Protoc 2009;4(3):309-24
  • Pickl M, Ries CH. Comparison of 3D and 2D tumor models reveals enhanced HER2 activation in 3D associated with an increased response to trastuzumab. Oncogene 2009;28(3):461-8
  • Cheng K, Lai Y, Kisaalita WS. Three-dimensional polymer scaffolds for high throughput cell-based assay systems. Biomaterials 2008;29(18):2802-12

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.