Issue 2, 2007

High-throughput screening of enzyme inhibition using an inhibitor gradient generated in a microchannel

Abstract

A new rapid microfluidic method for measuring enzyme inhibition is presented. The assay relies upon the creation of a uniform concentration of substrate and a microfluidically generated concentration gradient of inhibitor using a single microchannel and a single initial inhibitor concentration. The IC50 values of two enzyme inhibitors were determined using the new technique and validated using a conventional microtiter plate assay. Using both experimental and computational simulation techniques, the assay was shown to be sensitive to inhibitor potency and the distribution of inhibitor in the system. The method has the potential to be more accurate than conventional methods because of the comparatively large amount of data that may be collected. Recommendations for use of the assay are provided, including its use for high-throughput screening in drug discovery and general use in measurement of enzyme inhibition.

Graphical abstract: High-throughput screening of enzyme inhibition using an inhibitor gradient generated in a microchannel

Article information

Article type
Paper
Submitted
21 Jun 2006
Accepted
20 Sep 2006
First published
23 Oct 2006

Lab Chip, 2007,7, 249-255

High-throughput screening of enzyme inhibition using an inhibitor gradient generated in a microchannel

E. Garcia, M. S. Hasenbank, B. Finlayson and P. Yager, Lab Chip, 2007, 7, 249 DOI: 10.1039/B608789B

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