Review article: High-throughput screening: the hits and leads of drug discovery- an overview.
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Date
2011-03
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Abstract
The mechanism-based approach which corresponds to the target-based approach screens for
compounds with a specific mode of action. The highly effective nature of high-throughput
screening (HTS) for identification of highly target specific compounds is attributed to its precise
focus on single mechanism. This logical development of receptor technology is closely
connected with the changes in strategy of chemical synthesis. The vast number of compounds
produced by combinatorial chemistry and the possibility of testing many compounds, including
natural products, in a short period of time by HTS attracted attention of many workers. Various
detection techniques like fluorescence resonance energy transfer (FRET), Homogeneous time
resolved fluorescence (HTRF), etc are available, and the screening of more than 100,000
samples per day is possible. With the introduction of robotics, automation and miniaturization
techniques, it became feasible to screen 50,000 compounds a day with complex work-stations.
High-throughput screening methods are also used to characterize metabolic and pharmacokinetic
data about new drugs. With the use of Cassette dosing techniques even the pharmacokinetic data
can be assessed for large number of drug candidates, though not free of drawbacks, yet an
effective technique to further increase the drug discovery and development rate. The objective of
this article is to give an overview to the High-Throughput screening methodologies used in
industries as well as in academic research programmes.
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Keywords
High-Throughput Screening (HTS), Automation and Robotics, Miniaturization, Zfactor, Profiling, Errors
Citation
Martis E A, Radhakrishnan R, Badve R R. Review article: High-throughput screening: the hits and leads of drug discovery- an overview. Journal of Applied Pharmaceutical Science. 2011 Mar; 1(1): 2-10.