Emerging trends in high-throughput screening.

Novel technologies are emerging for high-throughput screening, driven by the needs and fine-tuning of established drug discovery activities, as well as by the emergence of novel target classes resulting from the deciphering of the human genome. Disciplines other than biology have now entered the screening scene, as bioinformatics, micro-technology and analytics provide powerful methodologies and applications that were not previously suitable for high-throughput screening. Many of these will move high-throughput screening from a numbers game to a content- and information-based approach to identify leads for novel disease targets.

[1]  John Davies,et al.  Design of small molecule libraries for NMR screening and other applications in drug discovery. , 2002, Current topics in medicinal chemistry.

[2]  T. Chiba,et al.  Exploring the protein interactome using comprehensive two-hybrid projects. , 2001, Trends in biotechnology.

[3]  Gary D Bader,et al.  Systematic Genetic Analysis with Ordered Arrays of Yeast Deletion Mutants , 2001, Science.

[4]  Martin Vogtherr,et al.  NMR-based screening methods for lead discovery. , 2003, EXS.

[5]  H. Blau,et al.  Monitoring protein-protein interactions in live mammalian cells by beta-galactosidase complementation. , 2000, Methods in enzymology.

[6]  Marina Veronesi,et al.  Fluorine-NMR competition binding experiments for high-throughput screening of large compound mixtures. , 2002, Combinatorial chemistry & high throughput screening.

[7]  S. Rees,et al.  Application of β-Galactosidase Enzyme Complementation Technology as a High Throughput Screening Format for Antagonists of the Epidermal Growth Factor Receptor , 2001 .

[8]  Ajay,et al.  Designing libraries with CNS activity. , 1999, Journal of medicinal chemistry.

[9]  H. Blau,et al.  Protein–protein interactions monitored in mammalian cells via complementation of β-lactamase enzyme fragments , 2002, Proceedings of the National Academy of Sciences of the United States of America.

[10]  K. Comess,et al.  Complex Gel Permeation Assays for Screening Combinatorial Libraries , 2001, Journal of biomolecular screening.

[11]  Rudi Verbeeck,et al.  Outlier Mining in High Throughput Screening Experiments , 2002, Journal of biomolecular screening.

[12]  H. Blau,et al.  Interaction blues: protein interactions monitored in live mammalian cells by beta-galactosidase complementation. , 2000, Trends in cell biology.

[13]  Mitchell A. Miller Chemical database techniques in drug discovery , 2002, Nature Reviews Drug Discovery.

[14]  T. Kenakin,et al.  Quantitative Molecular Pharmacology and Informatics in Drug Discovery , 2000 .

[15]  J. Kofron,et al.  Application of Micro Arrayed Compound Screening (pcARCS) to Identify Inhibitors of Caspase-3 , 2002, Journal of biomolecular screening.

[16]  J Mestres Virtual screening: a real screening complement to high-throughput screening. , 2002, Biochemical Society transactions.

[17]  Derek J Trezise,et al.  IonWorks™ HT: A New High-Throughput Electrophysiology Measurement Platform , 2003, Journal of biomolecular screening.

[18]  T. Garyantes,et al.  Development and Evaluation of High Throughput Functional Assay Methods for hERG Potassium Channel , 2001, Journal of biomolecular screening.

[19]  J. Drews Drug discovery: a historical perspective. , 2000, Science.

[20]  R. Eglen,et al.  Beta galactosidase enzyme fragment complementation as a novel technology for high throughput screening. , 2003, Combinatorial chemistry & high throughput screening.

[21]  M. Palmer,et al.  Cell-Based High-Throughput Screening Assay System for Monitoring G Protein-Coupled Receptor Activation Using β-Galactosidase Enzyme Complementation Technology , 2002, Journal of biomolecular screening.

[22]  Qifeng Xue,et al.  Multiplexed enzyme assays in capillary electrophoretic single‐use microfluidic devices , 2001, Electrophoresis.

[23]  J. Kofron,et al.  Microarray Compound Screening (μARCS) to Identify Inhibitors of HIV Integrase , 2002 .

[24]  P. Hajduk,et al.  Integration of NMR and high-throughput screening. , 2002, Combinatorial chemistry & high throughput screening.

[25]  Ye Fang,et al.  Membrane protein microarrays. , 2002, Journal of the American Chemical Society.

[26]  J. Mason,et al.  New 4-point pharmacophore method for molecular similarity and diversity applications: overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures. , 1999, Journal of medicinal chemistry.

[27]  J. Greef,et al.  Mass spectrometry–based bioassay for the screening of soluble orphan receptors , 2001 .

[28]  Ruedi Stoop,et al.  An Ontology for Pharmaceutical Ligands and Its Application for in Silico Screening and Library Design , 2002, J. Chem. Inf. Comput. Sci..

[29]  Jeremy L Jenkins,et al.  Virtual screening to enrich hit lists from high‐throughput screening: A case study on small‐molecule inhibitors of angiogenin , 2002, Proteins.

[30]  Didier Rognan,et al.  Protein‐based virtual screening of chemical databases. II. Are homology models of g‐protein coupled receptors suitable targets? , 2002, Proteins.

[31]  Charles J. Manly,et al.  The impact of informatics and computational chemistry on synthesis and screening. , 2001, Drug discovery today.

[32]  Ye Fang,et al.  G‐Protein‐Coupled Receptor Microarrays , 2002, Chembiochem : a European journal of chemical biology.

[33]  J. van der Greef,et al.  Potential of on-line micro-LC immunochemical detection in the bioanalysis of cytokines. , 2001, Journal of pharmaceutical and biomedical analysis.

[34]  S. Frantz,et al.  New drug approvals for 2002 , 2003, Nature Reviews Drug Discovery.

[35]  Claudio Dalvit,et al.  Fluorine-NMR experiments for high-throughput screening: theoretical aspects, practical considerations, and range of applicability. , 2003, Journal of the American Chemical Society.

[36]  Michael Fejtl,et al.  The roboocyte: automated cDNA/mRNA injection and subsequent TEVC recording on Xenopus oocytes in 96-well microtiter plates. , 2003, Receptors & channels.

[37]  R. Moaddel,et al.  Immobilized nicotinic receptor stationary phases: going with the flow in high-throughput screening and pharmacological studies. , 2003, Journal of pharmaceutical and biomedical analysis.

[38]  Alexander Tropsha,et al.  Rational principles of compound selection for combinatorial library design. , 2002, Combinatorial chemistry & high throughput screening.

[39]  Victor S. Lobanov,et al.  High-Density Miniaturized Thermal Shift Assays as a General Strategy for Drug Discovery , 2001 .

[40]  Jürgen Bajorath,et al.  Integration of virtual and high-throughput screening , 2002, Nature Reviews Drug Discovery.

[41]  R. Eglen,et al.  A High-Throughput, Nonisotopic, Competitive Binding Assay for Kinases Using Nonselective Inhibitor Probes (ED-NSIP™) , 2002, Journal of biomolecular screening.

[42]  Kurt Wüthrich,et al.  Nmr in drug discovery , 2002, Nature Reviews Drug Discovery.

[43]  R. Ozawa,et al.  A comprehensive two-hybrid analysis to explore the yeast protein interactome , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[44]  K L Spear,et al.  Retrospective analysis of an experimental high-throughput screening data set by recursive partitioning. , 2001, Journal of combinatorial chemistry.

[45]  H. Irth,et al.  High Resolution Screening of Plant Natural Product Extracts for Estrogen Receptor a and f3 Binding Activity Using an Online HPLC-MS Biochemical Detection System , 2001, Journal of biomolecular screening.

[46]  S. Pochapsky,et al.  Nuclear magnetic resonance as a tool in drug discovery, metabolism and disposition. , 2001, Current topics in medicinal chemistry.

[47]  Stanley Fields,et al.  A yeast sensor of ligand binding , 2001, Nature Biotechnology.

[48]  T. Garyantes,et al.  Identification of Gap Junction Blockers Using Automated Fluorescence Microscopy Imaging , 2003, Journal of biomolecular screening.