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Updated: Sep 25, 2026

Caspase-3 Activity in the Rat Amygdala Measured by Spectrofluorometry After Myocardial Infarction
Published on: January 12, 2016
Nicotinyl aspartyl ketones as inhibitors of caspase-3
Elise Isabel1, W Cameron Black, Christopher I Bayly
1Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada & Co., Pointe-Claire-Dorval, H9R 4P8, Quebec, Canada. elise_isabel@merck.com
Abstract:
Caspase-3 is a cysteinyl protease that mediates apoptotic cell death. Its inhibition may have an important impact in the treatment of several degenerative diseases. Since P(1) aspartic acid is a required element of recognition for this enzyme, a library of capped aspartyl aldehydes was synthesized using solid-phase chemistry. The 5-bromonicotinamide derivative of the aspartic acid aldehyde was identified to be an inhibitor of caspase-3. Substitution at the 5-position of the pyridine ring and conversion of the aldehyde to ketones led to a series of potent inhibitors of caspase-3.
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