Peptide methyl ketones as reversible inhibitors of cysteine proteinases

Journal of Enzyme Inhibition
D BrömmeS Fittkau

Abstract

Peptide methyl ketones represent a new class of reversible, competitive cysteine proteinase inhibitor with little or no effect on serine proteinases. The affinity of the inhibitors to papain (EC 3.4.22.3), cathepsin B (EC 3.4.22.1) and cathepsin L (EC 3.4.22.15) depends on the peptide chain length and on side-chain effects. Variations in the P1 and P4 positions (terminology of Schechter and Berger) and their influence on the efficiency of the inhibitors have been investigated. The most effective inhibitors display inhibition constants in the micromolar range. In contrast to the endopeptidases papain and the cathepsins B and L, the aminoendopeptidase cathepsin H (EC 3.4.22.16) is not inhibited by N-acylated peptide methyl ketones but only by amino methyl ketones containing a free alpha-amino group. The endopeptidases are not affected by amino methyl ketones.

References

Apr 1, 1977·European Journal of Biochemistry·H KirschkeP Bohley
Jan 1, 1976·Analytical Biochemistry·M ZimmermanG Patel
Sep 6, 1968·Biochemical and Biophysical Research Communications·I Schechter, A Berger
Apr 15, 1983·Archives of Biochemistry and Biophysics·E ShawJ Ruscica
Jun 2, 1980·FEBS Letters·H J KärgelJ Langner
Jan 1, 1981·Methods in Enzymology·A J Barrett, H Kirschke

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Citations

Jan 1, 1990·Journal of Enzyme Inhibition·H U Demuth
May 1, 2007·Biochimica Et Biophysica Acta·Stephen B PorterWalter K Schmidt
Jan 1, 1991·Journal of Enzyme Inhibition·H U Demuth, F Nyberg
Nov 6, 2001·Journal of Biochemical and Biophysical Methods·G JahreisH Kirschke

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