Amino Acids and Peptides. XXXIX. Synthesis of iNoc-Gln-Val-Val-Ala-Ala-pNA and Its Action on Thiol Proteinases

Yoshio OKADA; Yuko TSUDA; Yu MU; Kenichi HIRANO; Hiroshi OKAMOTO; Yoshiko OKAMOTO; Hisao KAKEGAWA; Hitoshi MATSUMOTO; Toshio SATO

doi:10.1248/cpb.43.96

Amino Acids and Peptides. XXXIX. Synthesis of iNoc-Gln-Val-Val-Ala-Ala-pNA and Its Action on Thiol Proteinases

Yoshio OKADA, Yuko TSUDA, Yu MU, Kenichi HIRANO, Hiroshi OKAMOTO, Yoshiko OKAMOTO, Hisao KAKEGAWA, Hitoshi MATSUMOTO, Toshio SATO

Author information

Yoshio OKADA
Yuko TSUDA
Yu MU
Kenichi HIRANO
Hiroshi OKAMOTO
Yoshiko OKAMOTO
Hisao KAKEGAWA
Hitoshi MATSUMOTO
Toshio SATO
Author's Organization：
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University
Daiichi College of Pharmaceutical Sciences
Faculty of Pharmaceutical Sciences, Tokushima Bunri University
Faculty of Pharmaceutical Sciences, Tokushima Bunri University
Faculty of Pharmaceutical Sciences, Tokushima Bunri University

Keywords: Gln-Val-Val-Ala-Gly sequence, isonicotinyloxycarbonyl derivative, non-competitive inhibition, papain, cathepsin L

JOURNAL FREE ACCESS

1995 Volume 43 Issue 1 Pages 96-99

DOI https://doi.org/10.1248/cpb.43.96

Details

Abstract

Based on the results of X-ray analysis of the complex between Suc-Gln-Val-Val-Ala-Ala-pNA, a fairly potent thiol proteinase inhibitor, and papain, iNoc-Gln-Val-Val-Ala-Ala-pNA was designed and prepared and its inhibitory activity against thiol proteinases was examined. iNoc-Gln-Val-Val-Ala-Ala-pNA inhibited cathepsin L fairly specifically, although its potency is not high.

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