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Enzyme Assay Design for High-Throughput Screening
2009Enzymes continue to be a major drug target class for the pharmaceutical industry with high-throughput screening the approach of choice for identifying initial active chemical compounds. The development of fluorescent- or absorbance-based readouts typically remains the formats of choice for enzyme screens and a wealth of experience from both industry ...
Kevin P, Williams, John E, Scott
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High Throughput Receptor Screening Assays
2017The recent technical advances in functional expression of olfactory receptors (OR s) make full deorphanization of human OR repertoire a realistic objective. Such a global knowledge of the precise mechanisms of odorant/receptor pairings will represent a crucial step for the development of an accurate model of how human nose perceives its chemical ...
Alex Veithen +2 more
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High-Throughput Screening Assays for Lipolytic Enzymes
2017Screening is defined as the identification of hits within a large library of variants of an enzyme or protein with a predefined property. In theory, each variant present in the respective library needs to be assayed; however, to save time and consumables, many screening regimes involve a primary round to identify clones producing active enzymes.
Alexander, Fulton +4 more
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Complement C5a Receptor Assay for High Throughput Screening
Journal of Receptor Research, 1991The complement C5a receptor on U937 cells, a human histiocytic lymphoma cell line, stimulated with dibutyryl-cAMP have been stabilized for at least 3 months at a dilute, ready to use concentration. [125I]-Bolton Hunter labeled C5a, (recombinant, human) has been prepared by reverse phase HPLC to 2200 Ci/mmol. Using a filtration binding assay the Kd from
S R, Harris +4 more
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High-Throughput Screening Assay for Biological Hydrogen Production
Analytical Chemistry, 2008This paper describes a screening assay, compatible with high-throughput bioprospecting or molecular biology methods, for assessing biological hydrogen (H2) production. While the assay is adaptable to various physical configurations, we describe its use in a 96-well, microtiter plate format with a lower plate containing H2-producing cyanobacteria ...
Paul S, Schrader +2 more
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Complex phenotypic assays in high-throughput screening
Current Opinion in Chemical Biology, 2004High-throughput screening (HTS), systematically testing thousands of small molecules to find candidates for lead optimization, primarily involves exposure of purified proteins to arrayed collections of small molecules. More complex phenotypic assays, such as cell-based or whole-organism assays, traditionally have flanked HTS, preceding it to validate ...
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Introduction: Cell-Based Assays for High-Throughput Screening
2009Cell-based assays represent approximately half of all high-throughput screens (HTS) currently performed. Here we review the history and status of HTS, and summarize some of the challenges and benefits associated with the use of cell-based assays in HTS, drawing upon themes that will reemerge in subsequent chapters in this book.
W Frank, An, Nicola J, Tolliday
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Design and Implementation of High-Throughput Screening Assays
2016HTS remains at the core of the drug discovery process, and so it is critical to design and implement HTS assays in a comprehensive fashion involving scientists from the disciplines of biology, chemistry, engineering, and informatics. This requires careful consideration of many options and variables, starting with the choice of screening strategy and ...
David J, Powell +2 more
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High-Throughput Screening Assays for Dengue Antiviral Drug Development
2021Dengue is an arthropod-borne viral disease that has become endemic and a global threat in over 100 countries. The increase in prevalence would require a long-term measure to control outbreaks. Sanofi Pasteur has licensed the tetravalent dengue vaccine (Dengvaxia) in certain dengue endemic countries.
Shobana Gabriel, Jabanathan +2 more
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Fluorescence Assays for High-Throughput Screening of Protein Kinases
Combinatorial Chemistry & High Throughput Screening, 2003Protein kinases comprise one of the most important group of targets for drug discovery research today. Methods to identify novel kinase inhibitors by high-throughput screening have evolved rapidly in recent years. An important aspect is the availability of fluorescent probes that can be applied in a homogeneous, or mix-and-measure, assay format.
G J R, Zaman +3 more
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