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Potent peptide alpha-ketohydroxamate inhibitors of recombinant human calpain I
K A Josef1, F W Kauer, R Bihovsky
1Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380-4245, USA. kjosef@cephalon.com
Bioorganic & Medicinal Chemistry Letters
|September 12, 2001
Abstract:
A series of potent dipeptide and tripeptide alpha-ketohydroxamic esters was prepared as inhibitors of recombinant human calpain I. Compound 3c, a Cbz-Leu-Phe hydroxamate, displayed the greatest potency against calpain I (IC(50)=6nM), while two compounds, 3l and 3m, both possessing the Cbz-Leu-Leu-Phe sequence, were the most potent (IC(50)=0.2 microM) in a MOLT-4 cell assay.