Direct inhibitory effect of curcumin on Src and focal adhesion kinase activity.

Abstract:

:Curcumin (diferuloylmethane) is a well-known agent with anti-inflammatory, antioxidant, and anticarcinogenic properties. In this study, we observed that curcumin inhibited the kinase activity of v-Src, which led to a decrease in tyrosyl substrate phosphorylation of Shc, cortactin, and FAK. Our in vitro kinase experiment revealed that the inhibitory effect of curcumin on Src could be direct. Consistent with the abrogation of Src activity was the reduction of Src-Tyr-416 phosphorylation, Src-mediated Shc-Tyr-317 phosphorylation, decreased ERK activation, and cell proliferation in v-Src transformed cells. Remarkably, curcumin not only exerted its negative effect on FAK via the disappearance of Src-mediated FAK phosphorylation, but also directly inhibited its enzymatic activity. Concurrent to reduced cortactin tyrosyl phosphorylation and FAK kinase activity was the abolishment of v-Src-mediated cell mobility. To our knowledge, this is the first report indicating that curcumin can retard cellular growth and migration via downregulation of Src and FAK kinase activity.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Leu TH,Su SL,Chuang YC,Maa MC

doi

10.1016/j.bcp.2003.08.017

subject

Has Abstract

pub_date

2003-12-15 00:00:00

pages

2323-31

issue

12

eissn

0006-2952

issn

1873-2968

pii

S0006295203006579

journal_volume

66

pub_type

杂志文章