26. Profiling protein function with small molecule microarrays
    N. Winssinger, S. Ficarro, P. G. Schultz, J. L. Harris
    Proc. Natl. Acad. Sci. USA 2002, 99, 11139-11144

The regulation of protein function through posttranslational modification, local environment, and protein-protein interaction is critical to cellular function. The ability to analyze on a genome-wide scale protein functional activity rather than changes in protein abundance or structure would provide important new insights into complex biological processes. Herein, we report the application of a spatially addressable small molecule microarray to an activity-based profile of proteases in crude cell lysates. The potential of this small molecule-based profiling technology is demonstrated by the detection of caspase activation upon induction of apoptosis, characterization of the activated caspase, and inhibition of the caspase-executed apoptotic phenotype using the small molecule inhibitor identified in the microarray-based profile.

DOI : 10.1073/pnas.172286899 

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