The Experts below are selected from a list of 70572 Experts worldwide ranked by ideXlab platform

Michael Entzeroth - One of the best experts on this subject based on the ideXlab platform.

  • Overview of High-Throughput Screening.
    Current protocols in pharmacology, 2009
    Co-Authors: Michael Entzeroth, Horst Flotow, Peter Condron
    Abstract:

    High-Throughput Screening (HTS) is a key process used in drug discovery to identify hits from compound libraries that may become leads for medicinal chemistry optimization. This updated overview discusses the utilization of compound libraries, compounds derived from combinatorial and parallel synthesis campaigns and natural product sources; creation of mother and daughter plates; and compound storage, handling, and bar coding in HTS. The unit also presents an overview of established and emerging assay technologies (i.e., time-resolved fluorescence, fluorescence polarization, fluorescence-correlation spectroscopy, functional whole cell assays, and High-content assays) and their integration in automation hardware and IT systems. This revised unit provides updated descriptions of state-of-the-art instrumentation and technologies in this rapidly changing environment. The section on assay methodologies now also covers enzyme complementation assays and methods for High-Throughput Screening of ion channel activities. Finally, a section on criteria for assay robustness is included discussing the Z'-factor, which is now a widely accepted criterion for evaluation and validation of High Throughput Screening assays.

  • Current Protocols in Pharmacology - Overview of High‐Throughput Screening
    Current Protocols in Pharmacology, 2009
    Co-Authors: Michael Entzeroth, Horst Flotow, Peter Condron
    Abstract:

    High-Throughput Screening (HTS) is a key process used in drug discovery to identify hits from compound libraries that may become leads for medicinal chemistry optimization. This updated overview discusses the utilization of compound libraries, compounds derived from combinatorial and parallel synthesis campaigns and natural product sources; creation of mother and daughter plates; and compound storage, handling, and bar coding in HTS. The unit also presents an overview of established and emerging assay technologies (i.e., time-resolved fluorescence, fluorescence polarization, fluorescence-correlation spectroscopy, functional whole cell assays, and High-content assays) and their integration in automation hardware and IT systems. This revised unit provides updated descriptions of state-of-the-art instrumentation and technologies in this rapidly changing environment. The section on assay methodologies now also covers enzyme complementation assays and methods for High-Throughput Screening of ion channel activities. Finally, a section on criteria for assay robustness is included discussing the Z'-factor, which is now a widely accepted criterion for evaluation and validation of High Throughput Screening assays.

  • Current Protocols in Pharmacology - Overview on High‐Throughput Screening
    Current Protocols in Pharmacology, 2003
    Co-Authors: Michael Entzeroth
    Abstract:

    High-Throughput Screening (HTS) is a key process used in drug discovery to identify hits from compound libraries that may become leads for medicinal chemistry optimization. This updated overview discusses the utilization of compound libraries, compounds derived from combinatorial and parallel synthesis campaigns and natural product sources; creation of mother and daughter plates; and compound storage, handling, and bar coding in HTS. The unit also presents an overview of established and emerging assay technologies (i.e., time-resolved fluorescence, fluorescence polarization, fluorescence-correlation spectroscopy, functional whole cell assays, and High-content assays) and their integration in automation hardware and IT systems. This revised unit provides updated descriptions of state-of-the-art instrumentation and technologies in this rapidly changing environment. The section on assay methodologies now also covers enzyme complementation assays and methods for High-Throughput Screening of ion channel activities. Finally, a section on criteria for assay robustness is included discussing the Z′-factor, which is now a widely accepted criterion for evaluation and validation of High Throughput Screening assays. Curr. Protoc. Pharmacol. 44:9.4.1-9.4.27. © 2009 by John Wiley & Sons, Inc. Keywords: High-Throughput Screening; High-content assays; functional assays; data management; hit identification; lead optimization

  • Emerging trends in High-Throughput Screening.
    Current opinion in pharmacology, 2003
    Co-Authors: Michael Entzeroth
    Abstract:

    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.

Peter Condron - One of the best experts on this subject based on the ideXlab platform.

  • Overview of High-Throughput Screening.
    Current protocols in pharmacology, 2009
    Co-Authors: Michael Entzeroth, Horst Flotow, Peter Condron
    Abstract:

    High-Throughput Screening (HTS) is a key process used in drug discovery to identify hits from compound libraries that may become leads for medicinal chemistry optimization. This updated overview discusses the utilization of compound libraries, compounds derived from combinatorial and parallel synthesis campaigns and natural product sources; creation of mother and daughter plates; and compound storage, handling, and bar coding in HTS. The unit also presents an overview of established and emerging assay technologies (i.e., time-resolved fluorescence, fluorescence polarization, fluorescence-correlation spectroscopy, functional whole cell assays, and High-content assays) and their integration in automation hardware and IT systems. This revised unit provides updated descriptions of state-of-the-art instrumentation and technologies in this rapidly changing environment. The section on assay methodologies now also covers enzyme complementation assays and methods for High-Throughput Screening of ion channel activities. Finally, a section on criteria for assay robustness is included discussing the Z'-factor, which is now a widely accepted criterion for evaluation and validation of High Throughput Screening assays.

  • Current Protocols in Pharmacology - Overview of High‐Throughput Screening
    Current Protocols in Pharmacology, 2009
    Co-Authors: Michael Entzeroth, Horst Flotow, Peter Condron
    Abstract:

    High-Throughput Screening (HTS) is a key process used in drug discovery to identify hits from compound libraries that may become leads for medicinal chemistry optimization. This updated overview discusses the utilization of compound libraries, compounds derived from combinatorial and parallel synthesis campaigns and natural product sources; creation of mother and daughter plates; and compound storage, handling, and bar coding in HTS. The unit also presents an overview of established and emerging assay technologies (i.e., time-resolved fluorescence, fluorescence polarization, fluorescence-correlation spectroscopy, functional whole cell assays, and High-content assays) and their integration in automation hardware and IT systems. This revised unit provides updated descriptions of state-of-the-art instrumentation and technologies in this rapidly changing environment. The section on assay methodologies now also covers enzyme complementation assays and methods for High-Throughput Screening of ion channel activities. Finally, a section on criteria for assay robustness is included discussing the Z'-factor, which is now a widely accepted criterion for evaluation and validation of High Throughput Screening assays.

Paul A. Negulescu - One of the best experts on this subject based on the ideXlab platform.

  • Miniaturized FRET assays and microfluidics: key components for ultra-High-Throughput Screening.
    Drug discovery today, 1999
    Co-Authors: Lora Mere, Todd Bennett, Peter Coassin, Paul England, Brian D. Hamman, Timothy J. Rink, Susan Zimmerman, Paul A. Negulescu
    Abstract:

    Abstract Assay miniaturization applicable across a wide range of target classes, along with automation and process integration, are well-recognized goals for ultra-High-Throughput Screening on an industrial scale. This report summarizes the implementation of fluorescence resonance energy transfer (FRET)-based biochemical and cell-based assays in 3456-well NanoWell ™ assay plates using key components of Aurora's ultra-High-Throughput Screening system.

Steven A Sundberg - One of the best experts on this subject based on the ideXlab platform.

  • High Throughput and ultra High Throughput Screening solution and cell based approaches
    Current Opinion in Biotechnology, 2000
    Co-Authors: Steven A Sundberg
    Abstract:

    The trend towards assay miniaturization for High-Throughput and ultra-High-Throughput Screening continues to spur development of homogeneous, fluorescence-based assays in Higher density, smaller volume microplate formats. Recently, first-generation microfluidic devices have been designed for performing continuous-flow biochemical and cell-based assays. These devices provide orders-of-magnitude reduction in reagent consumption, and offer the potential for implementing High-Throughput Screening in formats that integrate up-front compound handling with unique assay functionality.

Jaap M. J. Den Toonder - One of the best experts on this subject based on the ideXlab platform.

  • Microfluidics for cell-based High Throughput Screening platforms—A review
    Analytica chimica acta, 2015
    Co-Authors: Qun Fang, Jaap M. J. Den Toonder
    Abstract:

    In the last decades, the basic techniques of microfluidics for the study of cells such as cell culture, cell separation, and cell lysis, have been well developed. Based on cell handling techniques, microfluidics has been widely applied in the field of PCR (Polymerase Chain Reaction), immunoassays, organ-on-chip, stem cell research, and analysis and identification of circulating tumor cells. As a major step in drug discovery, High-Throughput Screening allows rapid analysis of thousands of chemical, biochemical, genetic or pharmacological tests in parallel. In this review, we summarize the application of microfluidics in cell-based High Throughput Screening. The Screening methods mentioned in this paper include approaches using the perfusion flow mode, the droplet mode, and the microarray mode. We also discuss the future development of microfluidic based High Throughput Screening platform for drug discovery.