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Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer

Cited 39 time in Web of Science Cited 41 time in Scopus
Authors
Nam, Hyun-Jin; Kim, Hwang-Phill; Yoon, Young-Kwang; Hur, Hyung-Seok; Song, Sang-Hyun; Kim, Maeng-Sup; Lee, Gwan-Sun; Han, Sae-Won; Im, Seock-Ah; Kim, Tae-You; Oh, Do-Youn; Bang, Yung-Jue
Issue Date
2011-03
Citation
Cancer Letters, Vol.302 No.2, pp.155-165
Keywords
HM781-36BPan-HER inhibitorGastric cancerAntitumor activityChemotherapeutic agents
Abstract
Trastuzumab, a HER2 directed treatment has shown clinical benefit in HER2 amplified gastric cancer. This study demonstrated the potent antitumor activity of HM781-36B, a quinazoline-based irreversible pan-HER inhibitor, in HER2 amplified gastric cancer cells (SNU216 and N87) in vitro and in vivo. HM781-36B inhibited phosphorylation of HER family and downstream signaling molecules, and induced apoptosis and G1 arrest. Furthermore, HM781-36B exerted synergistic effects with chemotherapeutic agents in both HER2 amplified and HER2 non-amplified gastric cancer cells. Therefore, HM781-36B may be useful for the treatment of HER2 amplified gastric cancer alone or in combination with chemotherapeutic agents. (C) 2011 Elsevier Ireland Ltd. All rights reserved.
ISSN
0304-3835
URI
https://hdl.handle.net/10371/172959
DOI
https://doi.org/10.1016/j.canlet.2011.01.010
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College of Medicine/School of Medicine (의과대학/대학원)Internal Medicine (내과학전공)Journal Papers (저널논문_내과학전공)
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