References
- Feng Y, Mitchison TJ, Bender A, et al. Multi-parameter phenotypic profiling: using cellular effects to characterize small-molecule compounds. Nat Rev Drug Discov 2009;8(7):567-78
- Pomper MG, Lee JS. Small animal imaging in drug development. Curr Pharm Des 2005;11(25):3247-72
- Krutzik PO, Nolan GP. Fluorescent cell barcoding in flow cytometry allows high-throughput drug screening and signaling profiling. Nat Methods 2006;3(5):361-8
- Litwin VM, Marder P. Recent Advances in Flow Cytometry: Platforms, Tools and the Challenges for Data Analysis. In: Smith PJ, Edward R, Errington RJ, Editors. Flow cytometry in drug discovery and development. Wiley; Hoboken, NJ: 2011:23-54
- Dufort S, Sancey L, Wenk C, et al. Optical small animal imaging in the drug discovery process. Biochim Biophys Acta Biomembr 2010;1798(12):2266-73
- Bednar B, Ntziachristos V. Opto-acoustic imaging of drug discovery biomarkers. Curr Pharm Biotechnol 2012;13(11):2117-27
- Toseland CP. Fluorescent labeling and modification of proteins. J Chem Biol 2013;6(3):85-95
- Sinkeldam RW, Greco NJ, Tor Y. Fluorescent Analogs of Biomolecular Building Blocks: Design, Properties, and Applications. Chem Rev 2010;110(5):2579-619
- Zeigler MB, Allen PB, Chiu DT. Probing rotational viscosity in synaptic vesicles. Biophys J 2011;100(11):2846-51
- Levitt JA, Chung P-H, Kuimova MK, et al. Fluorescence anisotropy of molecular rotors. ChemPhysChem 2011;12(3):662-72
- Newman M, Josiah S. Utilization of fluorescence polarization and time resolved fluorescence resonance energy transfer assay formats for SAR studies: Src kinase as a model system. J Biomol Screen 2004;9(6):525-32
- Turek-Etienne TC, Lei M, Terracciano JS, et al. Use of red-shifted dyes in a fluorescence polarization AKT kinase assay for detection of biological activity in natural product extracts. J Biomol Screen 2004;9(1):52-61
- Davey AM, Walvick RP, Liu Y, et al. Membrane order and molecular dynamics associated with IgE receptor cross-linking in mast cells. Biophys J 2007;92(1):343-55
- Gough AH, Taylor DL. Fluorescence anisotropy imaging microscopy maps calmodulin binding during cellular contraction and locomotion. J Cell Biol 1993;121(5):1095-107
- Levitt JA, Matthews DR, Ameer-Beg SM, et al. Fluorescence lifetime and polarization-resolved imaging in cell biology. Curr Opin Biotechnol 2009;20(1):28-36
- Luchowski R, Sarkar P, Bharill S, et al. Fluorescence polarization standard for near infrared spectroscopy and microscopy. Appl Opt 2008;47(33):6257-65
- Pu Y, Wang WB, Das BB, et al. Time-resolved fluorescence polarization dynamics and optical imaging of Cytate: a prostate cancer receptor-targeted contrast agent. Appl Opt 2008;47(13):2281-9
- Baffou G, Kreuzer MP, Kulzer F, et al. Temperature mapping near plasmonic nanostructures using fluorescence polarization anisotropy. Opt Express 2009;17(5):3291-8
- Bertz A, Ehlers J-E, Wöhl-Bruhn S, et al. Mobility of green fluorescent protein in hydrogel-based drug-delivery systems studied by anisotropy and fluorescence recovery after photobleaching. Macromol Biosci 2013;13(2):215-26
- Owicki JC. Fluorescence polarization and anisotropy in high throughput screening: perspectives and primer. J Biomol Screen 2000;5(5):297-306
- Smith DS, Eremin SA. Fluorescence polarization immunoassays and related methods for simple, high-throughput screening of small molecules. Anal Bioanal Chem 2008;391(5):1499-507
- Vickers CJ, González-Páez GE, Umotoy JC, et al. Small-molecule procaspase activators identified using fluorescence polarization. ChemBioChem 2013;14(12):1419-22
- Baughman BM, Jake Slavish P, DuBois RM, et al. Identification of influenza endonuclease inhibitors using a novel fluorescence polarization assay. ACS Chem Biol 2012;7(3):526-34
- Haus P, Korbus M, Schröder M, et al. Identification of selective class II histone deacetylase inhibitors using a novel dual-parameter binding assay based on fluorescence anisotropy and lifetime. J Biomol Screen 2011;16(10):1206-16
- Alontaga AY, li Y, Chen C-H, et al. Design of high throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface. ACS Comb Sci 2015;17(4):239-46
- Owen B, McMurray C. Rapid method for measuring DNA binding to protein using fluorescence anisotropy. Protocol Exchange 2009. [Epub ahead of print]
- LiCata VJ, Wowor AJ. Applications of Fluorescence Anisotropy to the Study of Protein–DNA Interactions. In: John JC, William Detrich HIII, editors. Methods in Cell Biology. Academic Press, Waltham, MA, USA; 2008; p. 243-62
- Jameson DM, Ross JA. Fluorescence polarization/anisotropy in diagnostics and imaging. Chem Rev 2010;110(5):2685-708
- Yengo CM, Berger CL. Fluorescence anisotropy and resonance energy transfer: powerful tools for measuring real time protein dynamics in a physiological environment. Curr Opin Pharmacol 2010;10(6):731-7
- Lea WA, Simeonov A. Fluorescence polarization assays in small molecule screening. Expert Opin Drug Discov 2011;6(1):17-32
- Lakowicz JR. Principles of fluorescence spectroscopy. 3rd edition. Springer; New York: 2006. p. 954
- DeRose PC, Resch-Genger U. Recommendations for fluorescence instrument qualification: the new ASTM standard Guide. Anal Chem 2010;82(5):2129-33
- Perrin F. The fluorescence of solutions: Molecular induction, polarization and duration of emission and photochemistry. Ann Phys 1929;12:169-275
- Gustafson TP, Cao Q, Achilefu S, et al. Defining a polymethine dye for fluorescence anisotropy applications in the near-infrared spectral range. ChemPhysChem 2012;13(3):716-23
- Szmacinski H, Lakowicz JR. Depolarization of surface-enhanced fluorescence: an approach to fluorescence polarization assays. Anal Chem 2008;80(16):6260-6
- Zhegalova NG, He S, Zhou H, et al. Minimization of self-quenching fluorescence on dyes conjugated to biomolecules with multiple labeling sites via asymmetrically charged NIR fluorophores. Contrast Media Mol Imaging 2014;9(5):355-62
- Irving M. Steady-state polarization from cylindrically symmetric fluorophores undergoing rapid restricted motion. Biophys J 1996;70(4):1830-5
- Wurth C, Pauli J, Lochmann C, et al. Integrating sphere setup for the traceable measurement of absolute photoluminescence quantum yields in the near infrared. Anal Chem 2012;84(3):1345-52
- Berezin MY, Lee H, Akers W, et al. Ratiometric analysis of fluorescence lifetime for probing binding sites in albumin with near-infrared fluorescent molecular probes. Photochem Photobiol 2007;83(6):1371-8
- Jameson D, Mocz G. Fluorescence Polarization/Anisotropy Approaches to Study Protein-Ligand Interactions. In: Ulrich Nienhaus G, editor. Protein-Ligand Interactions. Humana Press, New York City, NY, USA; 2005. p. 301-22
- Cooper M, Ebner A, Briggs M, et al. Cy3B: improving the performance of cyanine dyes. J Fluoresc 2004;14(2):145-50
- Araya Y, Kasuga J-i, Toyota K, et al. Structure-based design and synthesis of fluorescent PPARalpha/delta co-agonist and its application as a probe for fluorescent polarization assay of PPARdelta ligands. Chem Pharm Bull (Tokyo) 2008;56(9):1357-9
- Matveeva EG, Rudolph A, Moll JR, et al. Structure-selective anisotropy assay for amyloid Beta oligomers. ACS Chem Neurosci 2012;3(11):982-7
- Sørensen TJ, Thyrhaug E, Szabelski M, et al. Azadioxatriangulenium (ADOTA(+)): A long fluorescence lifetime fluorophore for large biomolecule binding assay. Methods Appl Fluoresc 2013;1(2):025001
- Guo X-Q, Castellano FN, Li L, Lakowicz JR. Use of a long-lifetime Re(I) complex in fluorescence polarization immunoassays of high-molecular-weight analytes. Anal Chem 1998;70(3):632-7
- Turek-Etienne TC, Small EC, Soh SC, et al. Evaluation of fluorescent compound interference in 4 fluorescence polarization assays: 2 kinases, 1 protease, and 1 phosphatase. J Biomol Screen 2003;8(2):176-84
- Gerega A, Zolek N, Soltysinski T, et al. Wavelength-resolved measurements of fluorescence lifetime of indocyanine green. J Biomed Opt 2011;16(6):067010
- Hilderbrand SA, Weissleder R. Near-infrared fluorescence: application to in vivo molecular imaging. Curr Opin Chem Biol 2010;14(1):71-9
- Rurack K, Spieles M. Fluorescence quantum yields of a series of red and near-infrared dyes emitting at 600-1000 nm. Anal Chem 2011;83(4):1232-42
- Zhegalova NG, Aydt A, Wang ST, et al. Molecular thermometers for potential applications in thermal ablation procedures. Proc SPIE 2013;85960I-60I-9
- Zhegalova NG, Dergunov SA, Wang ST, et al. Design of Fluorescent Nanocapsules as Ratiometric Nanothermometers. Chem Eur J 2014;20(33):10292-7
- Kumbhakar M, Mukerjee T, Pal H. Temperature effect on the fluroescence anisotropy decay dynamics of coumarin-153 Dye in Triton-X-100 and Brij-35 miscellar solutions. Photochem Photobiol 2005;81(3):588-94
- Gustafson TP, Dergunov SA, Akers WJ, et al. Blood triggered rapid release porous nanocapsules. RSC Advances 2013;3(16):5547-55
- Anderson BJ, Larkin C, Guja K, et al. Using fluorophore-labeled oligonucleotides to measure affinities of protein-DNA interactions. Meth Enzymol 2008;450:253-72
- Veiksina S, Kopanchuk S, Rinken A. Budded baculoviruses as a tool for a homogeneous fluorescence anisotropy-based assay of ligand binding to G protein-coupled receptors: The case of melanocortin 4 receptors. Biochim Biophys Acta Biomembr 2014;1838(1 Part B):372-81
- Malo N, Hanley JA, Cerquozzi S, et al. Statistical practice in high-throughput screening data analysis. Nat Biotech 2006;24(2):167-75
- Sui Y, Wu Z. Alternative statistical parameter for high-throughput screening assay quality assessment. J Biomol Screen 2007;12(2):229-34
- Zhang J-H, Chung TDY, Oldenburg KR. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4(2):67-73
- Feau C, Arnold LA, Kosinski A, et al. A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors. J Biomol Screen 2009;14(1):43-8
- Souza-Fagundes EM, Frank AO, Feldkamp MD, et al. A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication protein A. Anal Biochem 2012;421(2):742-9
- Mahapatra L, Mao C, Andruska N, et al. High-throughput fluorescence anisotropy screen for inhibitors of the oncogenic mRNA binding protein, IMP-1. J Biomol Screen 2014;19(3):427-36
- Dahlin JL, Walters MA. The essential roles of chemistry in high-throughput screening triage. Future Med Chem 2014;6(11):1265-90
- Piper DR, Duff SR, Eliason HC, et al. Development of the predictor hERG fluorescence polarization assay using a membrane protein enrichment approach. Assay Drug Dev Technol 2008;6(2):213-23
- Fermini B, Fossa AA. The impact of drug-induced QT interval prolongation on drug discovery and development. Nat Rev Drug Discov 2003;2(6):439-47
- US Food and Drug Administration, Guidance for industry: S7B nonclinical evaluation of the potential for delayed ventricular repolarization (QT interval prolongation) by human pharmaceuticals, 2005. (2006)
- Dorn A, Hermann F, Ebneth A, et al. Evaluation of a high-throughput fluorescence assay method for herg potassium channel inhibition. J Biomol Screen 2005;10(4):339-47
- Deacon M, Singleton D, Szalkai N, et al. Early evaluation of compound QT prolongation effects: a predictive 384-well fluorescence polarization binding assay for measuring hERG blockade. J Pharmacol Toxicol Methods 2007;55(3):238-47
- Singleton DH, Boyd H, Steidl-Nichols JV, et al. Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel. J Med Chem 2007;50(13):2931-41
- Arslan Yildiz A, Kang C, Sinner EK. Biomimetic membrane platform containing hERG potassium channel and its application to drug screening. Analyst 2013;138(7):2007-12
- Berezin MY, Achilefu S. Fluorescence lifetime measurements and biological imaging. Chem Rev 2010;110(5):2641-84
- Alibhai D, Kelly DJ, Warren S, et al. Automated fluorescence lifetime imaging plate reader and its application to Förster resonant energy transfer readout of Gag protein aggregation. J Biophotonics 2013;6(5):398-408
- Suhling K, Siegel J, Lanigan PMP, et al. Time-resolved fluorescence anisotropy imaging applied to live cells. Opt Lett 2004;29(6):584-6
- Schroder GF, Alexiev U, Grubmuller H. Simulation of fluorescence anisotropy experiments: probing protein dynamics. Biophys J 2005;89(6):3757-70
- Kortkhonjia E, Brandman R, Zhou JZ, et al. Probing antibody internal dynamics with fluorescence anisotropy and molecular dynamics simulations. MAbs 2013;5(2):306-22
- Tirri ME, Huttunen RJ, Toivonen J, et al. Two-photon excitation in fluorescence polarization receptor-ligand binding assay. J Biomol Screen 2005;10(4):314-19
- Walsh G. Pharmaceuticals, biologics and biopharmaceuticals. Biopharmaceuticals: Biochemistry and Biotechnology, 2nd edition. John Wiley & Sons, Hoboken, NJ, USA; 2003:1-42
- Berezin MY. Design and Development of Theranostic Nanomedicines. In: Janjic JM, Bai M, editors. Nanotechnology for biomedical imaging and diagnostics: from nanoparticle design to clinical applications. Wiley; Hoboken, NJ: 2015:429-465
- Katsnelson A. Momentum grows to make ‘personalized’ medicine more ‘precise’. Nat Med 2013;19(3):249-9
- Dolsten M, Søgaard M. Precision medicine: an approach to R&D for delivering superior medicines to patients. Clin Transl Med 2012;1:7
- Fang X, Tan W. Aptamers generated from Cell-SELEX for molecular medicine: a chemical biology approach. Acc Chem Res 2010;43(1):48-57
- Keefe AD, Pai S, Ellington A. Aptamers as therapeutics. Nat Rev Drug Discov 2010;9(7):537-50
- Sundaram P, Kurniawan H, Byrne ME, et al. Therapeutic RNA aptamers in clinical trials. Eur J Pharm Sci 2013;48(1–2):259-71
- Zhao Q, Lv Q, Wang H. Aptamer fluorescence anisotropy sensors for adenosine triphosphate by comprehensive screening tetramethylrhodamine labeled nucleotides. Biosensors and Bioelectronics 2015;70:188-93
- Zhu Z, Ravelet C, Perrier S, et al. Single-stranded DNA binding protein-assisted fluorescence polarization aptamer assay for detection of small molecules. Anal Chem 2012;84(16):7203-11
- Gokulrangan G, Unruh JR, Holub DF, et al. DNA aptamer-based bioanalysis of IgE by fluorescence anisotropy. Anal Chem 2005;77(7):1963-70
- Apperson K, Karolin J, Martin RW, et al. Nanoparticle metrology standards based on the time-resolved fluorescence anisotropy of silica colloids. Meas Sci Technol 2009;20(2):025310
- Schwartz S, Fixler D, Popovtzer R, et al. Fluorescence life-time imaging and steady state polarization for examining binding of fluorophores to gold nanoparticles. J Biophotonics 2015. [ Epub ahead of print]
- Kumar R, Roy I, Ohulchanskyy TY, et al. Covalently dye-linked, surface-controlled, and bioconjugated organically modified silica nanoparticles as targeted probes for optical imaging. ACS Nano 2008;2(3):449-56
- Sahoo Y, Goodarzi A, Swihart MT, et al. Aqueous ferrofluid of magnetite nanoparticles: fluorescence labeling and magnetophoretic control. J Phys Chem B 2005;109(9):3879-85
- Yang R, Jin J, Chen Y, et al. Carbon nanotube-quenched fluorescent oligonucleotides: probes that fluoresce upon hybridization. J Am Chem Soc 2008;130(26):8351-8
- Nelson K, Winter P, Shokeen M, et al. Nanoparticles for Bioimaging. Nanotechnology for Biomedical Imaging and Diagnostics. John Wiley & Sons, Inc; 2014. p. 151-92
- Okamatsu M, Feng F, Ohyanagi T, et al. Fluorescence polarization-based assay using N-glycan-conjugated quantum dots for screening in hemagglutinin blockers for influenza A viruses. J Virol Methods 2013;187(2):390-4
- Zhang J, Tian J, He Y, et al. Protein-binding aptamer assisted signal amplification for the detection of influenza A (H1N1) DNA sequences based on quantum dot fluorescence polarization analysis. Analyst 2013;138(17):4722-7
- Ye BC, Yin BC. Highly sensitive detection of mercury(II) ions by fluorescence polarization enhanced by gold nanoparticles. Angew Chem Int Ed Engl 2008;47(44):8386-9
- Huang Y, Liu X, Zhang L, et al. Nicking enzyme and graphene oxide-based dual signal amplification for ultrasensitive aptamer-based fluorescence polarization assays. Biosensors and Bioelectronics 2015;63:178-84
- Yue Q, Shen T, Wang L, et al. A convenient sandwich assay of thrombin in biological media using nanoparticle-enhanced fluorescence polarization. Biosensors and Bioelectronics 2014;56:231-6
- Liu J, Wang C, Jiang Y, et al. Graphene signal amplification for sensitive and real-time fluorescence anisotropy detection of small molecules. Anal Chem 2013;85(3):1424-30
- Vishwasrao HD, Trifilieff P, Kandel ER. In vivo imaging of the actin polymerization state with two-photon fluorescence anisotropy. Biophys J 2012;102(5):1204-14
- Dubach JM, Vinegoni C, Mazitschek R, et al. In vivo imaging of specific drug–target binding at subcellular resolution. Nat Commun 2014;5:3946
- Hess ST, Girirajan TPK, Mason MD. Ultra-high resolution imaging by fluorescence photoactivation localization microscopy. Biophys J 2006;91(11):4258-72
- Gould TJ, Gunewardene MS, Gudheti MV, et al. Nanoscale imaging of molecular positions and anisotropies. Nat Meth 2008;5(12):1027-30
- Pavani SRP, DeLuca JG, Piestun R. Polarization sensitive, three-dimensional, single-molecule imaging of cells with a double-helix system. Opt Express 2009;17(22):19644-55
- Hafi N, Grunwald M, van den Heuvel LS, et al. Fluorescence nanoscopy by polarization modulation and polarization angle narrowing. Nat Methods 2014;11(5):579-84
- Aurora High Performance Microplates. Website of Brooks Automation, Inc., Available from: www.brooks.com/products/life-science-systems/consumables/aurora-high-performance-microplates
- Matthews DR, Fruhwirth GO, Weitsman G, et al. A multi-functional imaging approach to high-content protein interaction screening. PLoS ONE 2012;7(4):e33231
- Assay development guidelines for image-based high content screening, high content analysis and high content imaging in assay guidance manual. Buchser W, Collins M, Garyantes T, et al. editors. Eli Lilly & Company and the National Center for Advancing Translational Sciences, Bethesda, MD, 2012
- Schindelin J, Arganda-Carreras I, Frise E, et al. Fiji: an open-source platform for biological-image analysis. Nat Meth 2012;9(7):676-82
- Sailem HZ, Sero JE, Bakal C. Visualizing cellular imaging data using PhenoPlot. Nat Commun 2015;6
- Bosworth N, Towers P. Scintillation proximity assay. Nature 1989;341(6238):167-8
- Glickman JF, Schmid A, Ferrand S. Scintillation proximity assays in high-throughput screening. Assay Drug Dev Technol 2008;6(3):433-55
- Eglen RM, Reisine T, Roby P, et al. The use of AlphaScreen technology in HTS: Current status. Curr Chem Genomics 2008;1:2-10
- Cochran JN, Diggs PV, Nebane NM, et al. AlphaScreen HTS and live-cell bioluminescence resonance energy transfer (BRET) assays for identification of Tau-Fyn SH3 interaction inhibitors for Alzheimer disease. J Biomol Screen 2014;19(10):1338-49
- Ungermannova D, Lee J, Zhang G, et al. High-throughput screening AlphaScreen assay for identification of small-molecule inhibitors of ubiquitin E3 ligase SCFSkp2-Cks1. J Biomol Screen 2013;18(8):910-20
- Williams C. cAMP detection methods in HTS: selecting the best from the rest. Nat Rev Drug Discov 2004;3(2):125-35
- Thomsen W, Frazer J, Unett D. Functional assays for screening GPCR targets. Curr Opin Biotechnol 2005;16(6):655-65
- Zhang R, Xie X. Tools for GPCR drug discovery. Acta Pharm Sinic 2012;33(3):372-84
- Mayr LM, Bojanic D. Novel trends in high-throughput screening. Curr Opin Pharmacol 2009;9(5):580-8
- Baell J, Walters MA. Chemistry: Chemical con artists foil drug discovery. Nature 2014;513(7519):481-3
- Feng BY, Simeonov A, Jadhav A, et al. A high-throughput screen for aggregation-based inhibition in a large compound library. J Med Chem 2007;50(10):2385-90
- Lim SP, Wang Q-Y, Noble CG, et al. Ten years of dengue drug discovery: Progress and prospects. Antiviral Res 2013;100(2):500-19
- Catrow JL, Zhang Y, Zhang M, et al. Discovery of selective small-molecule inhibitors for the beta-catenin/T-cell factor protein-protein interaction through the optimization of the acyl hydrazone moiety. J Med Chem 2015;58(11):4678-92
- Møller EH, Fano M, van de Weert M, et al. Comparability of protein pharmaceuticals and the suitability of methods for secondary structure analysis. Pharmaceut Technol Europe 2006;38-42