Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 57, Issue 11, Pages 4969-4974Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm500345q
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Funding
- Northwestern University
- Pew Charitable Trusts
- NIH [1T32GM105538-01]
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A novel fragment-based drug discovery approach is reported which irreversibly tethers drug-like fragments to catalytic cysteines. We attached an electrophile to 100 fragments without significant alterations in the reactivity of the electrophile. A mass spectrometry assay discovered three nonpeptidic inhibitors of the cysteine protease papain. The identified compounds display the characteristics of irreversible inhibitors. The irreversible tethering system also displays specificity: the three identified papain inhibitors did not covalently react with UbcH7, USP08, or GST-tagged human rhinovirus 3C protease.
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