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High-Throughput Screening of Enzyme Inhibitors: Automatic Determination of Tight-Binding Inhibition Constants

✍ Scribed by Petr Kuzmič; Steve Sideris; Lynne M. Cregar; Kyle C. Elrod; Kenneth D. Rice; James W. Janc

Book ID
102561984
Publisher
Elsevier Science
Year
2000
Tongue
English
Weight
74 KB
Volume
281
Category
Article
ISSN
0003-2697

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✦ Synopsis

Determination of tight-binding inhibition constants by nonlinear least-squares regression requires sufficiently good initial estimates of the best-fit values.

Normally an initial estimate of the inhibition constant must be provided by the investigator. This paper describes an automatic procedure for the estimation of tight-binding inhibition constants directly from doseresponse data. Because the procedure does not require human intervention, it was incorporated into an algorithm for high-throughput screening of enzyme inhibitors. A suitable computer program is available electronically (http://www.biokin.com). Representative experimental data are shown for the inhibition of human mast-cell tryptase.

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