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ID: ALA1133264

Journal: Bioorg Med Chem Lett

Title: Development of peptidyl alpha-keto-beta-aldehydes as new inhibitors of cathepsin L--comparisons of potency and selectivity profiles with cathepsin B.

Authors: Lynas JF, Hawthorne SJ, Walker B.

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 alpha-keto-beta-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.

CiteXplore: 10937745

DOI: 10.1016/s0960-894x(00)00340-1