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Proc Natl Acad Sci U S A. 2002 Aug 20;99(17):11139-44. Epub 2002 Aug 7.

Profiling protein function with small molecule microarrays.

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1
Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.

Abstract

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.

PMID:
12167675
PMCID:
PMC123223
DOI:
10.1073/pnas.172286899
[Indexed for MEDLINE]
Free PMC Article
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