Significant effects of Z-Gln-Val-Val-OMe, common sequences of thiol proteinase inhibitors on thiol proteinases

The first studies on a series of the small synthetic thiol proteinase inhibitors, conservative common sequences in several thiol proteinase inhibitors, are described. Among the many interesting findings with synthetic thiol proteinase inhibitors was the observation that the most effective analogue,...

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Veröffentlicht in:Biochemical and biophysical research communications 1987-03, Vol.143 (2), p.749-752
Hauptverfasser: Teno, N., Tsuboi, S., Itoh, N., Okamoto, H., Okada, Y.
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container_end_page 752
container_issue 2
container_start_page 749
container_title Biochemical and biophysical research communications
container_volume 143
creator Teno, N.
Tsuboi, S.
Itoh, N.
Okamoto, H.
Okada, Y.
description The first studies on a series of the small synthetic thiol proteinase inhibitors, conservative common sequences in several thiol proteinase inhibitors, are described. Among the many interesting findings with synthetic thiol proteinase inhibitors was the observation that the most effective analogue, Z-Gln-Val-Val-Ala-Gly-OMe, whose amino and carboxyl groups were protected with Z and OMe, respectively, showed inhibitory activity on papain and cathepsin B and protected papain from egg cystatin, human low-molecular-weight kininogen and T-kininogen-induced inhibition but not from leupeptin-induced inhibition. Moreover, it was revealed that Z-Gln-Val-Val-OMe was the smallest peptide to exhibit a protective effect on papain.
doi_str_mv 10.1016/0006-291X(87)91417-3
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source MEDLINE; Elsevier ScienceDirect Journals
subjects Amino Acid Sequence
Animals
Applied sciences
Binding Sites
Binding, Competitive
Cathepsin B - antagonists & inhibitors
Cystatins
Exact sciences and technology
Kininogens - antagonists & inhibitors
Kininogens - pharmacology
Leupeptins - antagonists & inhibitors
Oligopeptides - chemical synthesis
Oligopeptides - metabolism
Oligopeptides - pharmacology
Other techniques and industries
Papain - antagonists & inhibitors
Protease Inhibitors
Proteins - pharmacology
Structure-Activity Relationship
title Significant effects of Z-Gln-Val-Val-OMe, common sequences of thiol proteinase inhibitors on thiol proteinases
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