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OPB-31121, a novel small molecular inhibitor, disrupts the JAK2/STAT3 pathway and exhibits an antitumor activity in gastric cancer cells.

Abstract：

:We investigated the mechanisms of action and antitumor effects of OPB-31121, a novel STAT3 inhibitor, in gastric cancer cells. OPB-31121 downregulated JAK2 and gp130 expression and inhibited JAK2 phosphorylation which leads to inhibition of STAT3 phosphorylation. OPB-31121 inhibited constitutively activated and IL-6-induced JAK/STAT signaling pathway. OPB-31121 decreased cell proliferation in both gastric cancer cells and in a xenograft model, induced the apoptosis of gastric cancer cells, inhibited the expression of antiapoptotic proteins, and showed synergism with 5-fluorouracil and cisplatin. Taken together, our study suggests that STAT3 inhibition with OPB-31121 can be tested in patients with gastric cancer.

journal_name

Cancer Lett

journal_title

Cancer letters

authors

Kim MJ,Nam HJ,Kim HP,Han SW,Im SA,Kim TY,Oh DY,Bang YJ

doi

10.1016/j.canlet.2013.02.010

subject

Has Abstract

pub_date

2013-07-10 00:00:00

pages

145-52

issue

1

eissn

0304-3835

issn

1872-7980

pii

S0304-3835(13)00122-5

journal_volume

335

pub_type

杂志文章

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