Vertebrate Collagenase Inhibitor. I. : Tripeptidyl Hydroxamic Acids

Shinjiro ODAKE; Toru OKAYAMA; Masami OBATA; Tadanori MORIKAWA; Shunji HATTORI; Hisae HORI; Yutaka NAGAI

doi:10.1248/cpb.38.1007

Shinjiro ODAKE, Toru OKAYAMA, Masami OBATA, Tadanori MORIKAWA, Shunji HATTORI, Hisae HORI, Yutaka NAGAI

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Keywords: collagenase, hydroxamic acid, inhibitor, peptide synthesis, tripeptide

JOURNAL FREE ACCESS

1990 Volume 38 Issue 4 Pages 1007-1011

DOI https://doi.org/10.1248/cpb.38.1007

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Abstract

A series of tripeptidyl analogues carrying hydroxamic acid residue at the C-terminus of the molecule were synthesized, and their inhibitory activities against vertebrate collagenase and other metalloenzymes including bacterial collagenase were examined. Both Z-Pro-Leu-Ala-NHOH and Z-Pro-D-Leu-D-Ala-NHOH showed highly specific and potent inhibitory activity against tadpole and human skin collagenases with an IC₅₀ of 10^-6 M order.

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