Journal
LAB ON A CHIP
Volume 7, Issue 2, Pages 249-255Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/b608789b
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Funding
- NIDCR NIH HHS [T32-DE07023] Funding Source: Medline
- NATIONAL INSTITUTE OF DENTAL &CRANIOFACIAL RESEARCH [T32DE007023] Funding Source: NIH RePORTER
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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.
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