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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

Cited 72 time in Web of Science Cited 78 time in Scopus
Authors
Kim, Mi-Jung; Nam, Hyun-Jin; Kim, Hwang-Phill; Han, Sae-Won; Im, Seock-Ah; Kim, Tae-You; Oh, Do-Youn; Bang, Yung-Jue
Issue Date
2013-07
Citation
Cancer Letters, Vol.335 No.1, pp.145-152
Keywords
OPB-31121Gastric cancerSTAT3JAK2IL-6
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. (c) 2013 Elsevier Ireland Ltd. All rights reserved.
ISSN
0304-3835
URI
https://hdl.handle.net/10371/173104
DOI
https://doi.org/10.1016/j.canlet.2013.02.010
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College of Medicine/School of Medicine (의과대학/대학원)Internal Medicine (내과학전공)Journal Papers (저널논문_내과학전공)
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