Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 3, Issue 5, Pages 422-426Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml300056y
Keywords
NAAA; cysteine amidase; covalent inhibitors; high resolution mass spectrometry; proteomics
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Funding
- Istituto Italiano di Tecnologia
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The cysteine amidase N-acylethanolamine acid amidase (NAAA) is a member of the N-terminal nucleophile class of enzymes and a potential target for anti-inflammatory drugs. We investigated the mechanism of inhibition of human NAAA by substituted beta-lactones. We characterized pharmacologically a representative member of this class, ARN077, and showed, using high-resolution liquid chromatography-tandem mass spectrometry, that this compound forms a thioester bond with the N-terminal catalytic cysteine in human NAAA.
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