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PKC412 induces apoptosis through a caspase-dependent mechanism in human keloid-derived fibroblasts.

Abstract：

:There is no established pharmacological therapy for skin keloids, a wound healing disorder. In this study, we investigated the effect of N-benzoyl staurosporine (PKC412), a protein kinase C inhibitor, on human keloid-derived fibroblasts to examine whether this agent is applicable for the treatment of keloid formation. Although PKC412 induced apoptosis in keloid fibroblasts in a time- and dose-dependent manner, the effective concentration of this agent was much higher than that of staurosporine. Western blotting showed that both PKC412 (10 microM) and staurosporine (100 nM) cleaved pro-caspase-3 to active forms. An in vitro caspase assay also showed that PKC412 and staurosporine elevated caspase-3 activities. Carbobenzoxy-Val-Ala-Asp-fluoromethyl ketone (Z-VAD-FMK), a caspase inhibitor with a broad spectrum, inhibited caspase-3 activities stimulated by PKC412 and staurosporine; however, only PKC412-induced apoptosis, but not staurosporine-induced apoptosis, was prevented by Z-VAD-FMK. These results suggested that PKC412-induced apoptosis, but not staurosporine-induced apoptosis, is mainly mediated by the caspase-dependent mechanism.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Nakazono-Kusaba A,Takahashi-Yanaga F,Miwa Y,Morimoto S,Furue M,Sasaguri T

doi

10.1016/j.ejphar.2004.06.050

keywords:

subject

Has Abstract

pub_date

2004-08-23 00:00:00

pages

155-60

issue

2

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(04)00691-0

journal_volume

497

pub_type

杂志文章

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