1215015-96-5Relevant articles and documents
Noncovalent tripeptidyl benzyl- And cyclohexyl-amine inhibitors of the cysteine protease caspase-1
L?ser, Reik,Abbenante, Giovanni,Madala, Praveen K.,Halili, Maria,Le, Giang T.,Fairlie, David P.
supporting information; experimental part, p. 2651 - 2655 (2010/08/20)
Potent and noncovalent inhibitors of caspase-1 were produced by incorporating a secondary amine (reduced amide) isostere in place of the conventional electrophile (e.g., aldehyde) that normally confers high potency to cysteine protease inhibitors. Benzyl- or cyclohexylamines produced potent, reversible, and competitive inhibitors that were selective for caspase-1 (e.g., Ki = 47 nM) over caspases 3 and 8 with minimal cytotoxicity. Unlike most cysteine protease inhibitors, these compounds do not react covalently and indiscriminately with thiols.
