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- Title
High Throughput Screening via Mass Spectrometry: A Case Study Using Acetylcholinesterase.
- Authors
Can C. Özbal; William A. LaMarr; John R. Linton; Donald F. Green; Arrin Katz; Thomas B. Morrison; Colin J.H. Brenan
- Abstract
Mass spectrometry-based screening can be applied to a wide range of targets, includingthose intractable targets that use substrates such as lipids, fatty acids, phospholipids, steroids,prostaglandins, and other compounds not generally amenable to conventional screening techniques.The major limitation to this approach is throughput, making HTS via mass spectrometry impractical.We present a mass spectrometry-based technique and hardware for lead discovery applications. Massspectrometry enables the design of label-free assays using biologically native substrates for a widerange of enzymatic targets. This system can be used for the direct quantification of analytes incomplex reaction mixtures with typical throughputs of 4–5 s per sample. A mass spectrometrybasedassay was developed to identify inhibitors of acetylcholinesterase, an enzyme with clinicalimportance in Alzheimer's disease. The system was used to screen a small chemical library. Severalpotent inhibitors were identified, and the IC50 values of the inhibitors were determined.
- Publication
Assay & Drug Development Technologies, 2004, Vol 2, Issue 4, p373
- ISSN
1540-658X
- Publication type
Article