Abstract

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"High-throughput screening of enzyme inhibitors: Automatic determination of tight-binding inhibition constants" Kuzmic, P.; Sideris, S; Cregar, L.M.; Elrod, K.C.; Rice, K.D.; and Janc, J.W. (2000) Anal. Biochem. 281, 62-67. Abstract: 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 dose-response 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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