Abstract
A surface-based laser desorption/ionization mass spectrometry assay that makes use of Desorption/Ionization on Silicon Mass Spectrometry (DIOS-MS) has been developed to monitor enzyme activity and enzyme inhibition. DIOS-MS has been used to characterize inhibitors from a library and then to monitor their activity against selected enzyme targets, including proteases, glycotransferase, and acetylcholinesterase. An automated DIOS-MS system was also used as a high-throughput screen for the activity of novel enzymes and enzyme inhibitors. On two different commercially available instruments, a sampling rate of up to 38 inhibitors per minute was accomplished, with thousands of inhibitors being monitored. The ease of applying mass spectrometry toward developing enzyme assays and the speed of surface-based assays such as DIOS for monitoring inhibitor effectiveness and enzyme activity makes it attractive for a broad range of screening applications.
Original language | English |
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Pages (from-to) | 921-927 |
Number of pages | 7 |
Journal | ChemBioChem |
Volume | 5 |
Issue number | 7 |
DOIs | |
Publication status | Published - 5 Jul 2004 |
Externally published | Yes |
Keywords
- DIOS
- Enzymes
- High-throughput screening
- Inhibitors
- Plate reader
ASJC Scopus subject areas
- Drug Discovery
- Organic Chemistry
- Biochemistry, Genetics and Molecular Biology(all)