Development of peptidyl α-keto-β-aldehydes as new inhibitors of cathepsin L - Comparisons of potency and selectivity profiles with cathepsin B

J.F. Lynas, S.J. Hawthorne, B. Walker

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Abstract

We have utilized previously known substrate and inhibitor specificity profiles for the lysosomal cysteine protease, cathepsin L, to design a new series of putative inhibitors of this enzyme, based on di- and tri-peptidyl α-keto-β-aldehydes. Kinetic evaluation of these compounds revealed Z-Phe-Tyr(OBut)-COCHO, with a Ki=0.6 nM, to be the most potent, synthetic reversible inhibitor of cathepsin L reported to date
Original languageEnglish
Pages (from-to)1771-1773
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume10
Issue number15
DOIs
Publication statusPublished - 2000

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