New fluorescence techniques for high-throughput drug discovery.

The rapid increase of compound libraries as well as new targets emerging from the Human Genome Project require constant progress in pharmaceutical research. An important tool is High-Throughput Screening (HTS), which has evolved as an indispensable instrument in the pre-clinical target-to-IND (Inves...

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主要な著者: Jäger, S, Brand, L, Eggeling, C
フォーマット: Journal article
言語:English
出版事項: 2003
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author Jäger, S
Brand, L
Eggeling, C
author_facet Jäger, S
Brand, L
Eggeling, C
author_sort Jäger, S
collection OXFORD
description The rapid increase of compound libraries as well as new targets emerging from the Human Genome Project require constant progress in pharmaceutical research. An important tool is High-Throughput Screening (HTS), which has evolved as an indispensable instrument in the pre-clinical target-to-IND (Investigational New Drug) discovery process. HTS requires machinery, which is able to test more than 100,000 potential drug candidates per day with respect to a specific biological activity. This calls for certain experimental demands especially with respect to sensitivity, speed, and statistical accuracy, which are fulfilled by using fluorescence technology instrumentation. In particular the recently developed family of fluorescence techniques, FIDA (Fluorescence Intensity Distribution Analysis), which is based on confocal single-molecule detection, has opened up a new field of HTS applications. This report describes the application of these new techniques as well as of common fluorescence techniques--such as confocal fluorescence lifetime and anisotropy--to HTS. It gives experimental examples and presents advantages and disadvantages of each method. In addition the most common artifacts (auto-fluorescence or quenching by the drug candidates) emerging from the fluorescence detection techniques are highlighted and correction methods for confocal fluorescence read-outs are presented, which are able to circumvent this deficiency.
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spelling oxford-uuid:c212bae6-6c15-4de8-b99b-50877ed84ea32022-03-27T06:06:13ZNew fluorescence techniques for high-throughput drug discovery.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:c212bae6-6c15-4de8-b99b-50877ed84ea3EnglishSymplectic Elements at Oxford2003Jäger, SBrand, LEggeling, CThe rapid increase of compound libraries as well as new targets emerging from the Human Genome Project require constant progress in pharmaceutical research. An important tool is High-Throughput Screening (HTS), which has evolved as an indispensable instrument in the pre-clinical target-to-IND (Investigational New Drug) discovery process. HTS requires machinery, which is able to test more than 100,000 potential drug candidates per day with respect to a specific biological activity. This calls for certain experimental demands especially with respect to sensitivity, speed, and statistical accuracy, which are fulfilled by using fluorescence technology instrumentation. In particular the recently developed family of fluorescence techniques, FIDA (Fluorescence Intensity Distribution Analysis), which is based on confocal single-molecule detection, has opened up a new field of HTS applications. This report describes the application of these new techniques as well as of common fluorescence techniques--such as confocal fluorescence lifetime and anisotropy--to HTS. It gives experimental examples and presents advantages and disadvantages of each method. In addition the most common artifacts (auto-fluorescence or quenching by the drug candidates) emerging from the fluorescence detection techniques are highlighted and correction methods for confocal fluorescence read-outs are presented, which are able to circumvent this deficiency.
spellingShingle Jäger, S
Brand, L
Eggeling, C
New fluorescence techniques for high-throughput drug discovery.
title New fluorescence techniques for high-throughput drug discovery.
title_full New fluorescence techniques for high-throughput drug discovery.
title_fullStr New fluorescence techniques for high-throughput drug discovery.
title_full_unstemmed New fluorescence techniques for high-throughput drug discovery.
title_short New fluorescence techniques for high-throughput drug discovery.
title_sort new fluorescence techniques for high throughput drug discovery
work_keys_str_mv AT jagers newfluorescencetechniquesforhighthroughputdrugdiscovery
AT brandl newfluorescencetechniquesforhighthroughputdrugdiscovery
AT eggelingc newfluorescencetechniquesforhighthroughputdrugdiscovery