DC Field | Value | Language |
---|---|---|
dc.contributor.author | Yun, Sun-Mi | ko |
dc.contributor.author | Lee, Ju-Hee | ko |
dc.contributor.author | Jung, Kyung Hee | ko |
dc.contributor.author | Lee, Hyunseung | ko |
dc.contributor.author | Lee, Soyoung | ko |
dc.contributor.author | Hong, Sungwoo | ko |
dc.contributor.author | Hong, Soon-Sun | ko |
dc.date.accessioned | 2013-08-14T01:09:20Z | - |
dc.date.available | 2013-08-14T01:09:20Z | - |
dc.date.created | 2013-08-09 | - |
dc.date.created | 2013-08-09 | - |
dc.date.issued | 2013-07 | - |
dc.identifier.citation | INTERNATIONAL JOURNAL OF ONCOLOGY, v.43, no.1, pp.201 - 209 | - |
dc.identifier.issn | 1019-6439 | - |
dc.identifier.uri | http://hdl.handle.net/10203/175026 | - |
dc.description.abstract | The phosphatidylinositol 3-kinase (PI3K) pathway plays a central role in cell proliferation and survival in human cancer and is emerging as an attractive therapeutic target. In this study, we synthesized a novel PI3K alpha inhibitor, HS-159 [N-(5-(3-(3-cyanophenyl)imidazo[1,2-a]pyridin-6-yl)pyridin-3-yl)benzenesulfonamide] and evaluated its anticancer effects on Huh-7 human hepatocellular carcinoma (HCC) cells. HS-159 effectively inhibited the phosphorylation of downstream PI3K effectors such as Akt, mTOR and P70S6 kinases in a dose-dependent manner. This compound also induced apoptosis and increased the fraction of apoptotic cells in the sub-G(1) phase as well as the levels of cleaved PARP, caspase-3 and -9. Furthermore, HS-159 decreased the expression of hypoxia inducible factor-1 alpha and vascular endothelial growth factor which play important roles in angiogenesis. The anti-angiogenic effect of HS-159 was confirmed by the suppression of tube formation and migration of human umbilical vein endothelial cells in vitro. Collectively, our results demonstrate that HS-159 exhibited anticancer activities including the induction of apoptosis and inhibition of angiogenesis by blocking the PI3K/Akt pathway in Huh-7 cells. Therefore, we suggest that this drug may be potentially used for targeted HCC therapy. | - |
dc.language | English | - |
dc.publisher | SPANDIDOS PUBL LTD | - |
dc.subject | HYPOXIA-INDUCIBLE FACTOR-1 | - |
dc.subject | ENDOTHELIAL GROWTH-FACTOR | - |
dc.subject | CANCER-THERAPY | - |
dc.subject | ANTITUMOR-ACTIVITY | - |
dc.subject | BREAST-CANCER | - |
dc.subject | FACTOR-I | - |
dc.subject | PATHWAY | - |
dc.subject | TARGET | - |
dc.subject | AKT | - |
dc.subject | CELLS | - |
dc.title | Induction of apoptosis and suppression of angiogenesis of hepatocellular carcinoma by HS-159, a novel phosphatidylinositol 3-kinase inhibitor | - |
dc.type | Article | - |
dc.identifier.wosid | 000321023100024 | - |
dc.identifier.scopusid | 2-s2.0-84879615715 | - |
dc.type.rims | ART | - |
dc.citation.volume | 43 | - |
dc.citation.issue | 1 | - |
dc.citation.beginningpage | 201 | - |
dc.citation.endingpage | 209 | - |
dc.citation.publicationname | INTERNATIONAL JOURNAL OF ONCOLOGY | - |
dc.identifier.doi | 10.3892/ijo.2013.1912 | - |
dc.contributor.localauthor | Hong, Sungwoo | - |
dc.contributor.nonIdAuthor | Yun, Sun-Mi | - |
dc.contributor.nonIdAuthor | Lee, Ju-Hee | - |
dc.contributor.nonIdAuthor | Jung, Kyung Hee | - |
dc.contributor.nonIdAuthor | Lee, Hyunseung | - |
dc.contributor.nonIdAuthor | Lee, Soyoung | - |
dc.contributor.nonIdAuthor | Hong, Soon-Sun | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | phosphatidylinositol 3-kinase inhibitor | - |
dc.subject.keywordAuthor | anticancer | - |
dc.subject.keywordAuthor | apoptosis | - |
dc.subject.keywordAuthor | angiogenesis | - |
dc.subject.keywordAuthor | hepatocellular carcinoma | - |
dc.subject.keywordPlus | HYPOXIA-INDUCIBLE FACTOR-1 | - |
dc.subject.keywordPlus | ENDOTHELIAL GROWTH-FACTOR | - |
dc.subject.keywordPlus | CANCER-THERAPY | - |
dc.subject.keywordPlus | ANTITUMOR-ACTIVITY | - |
dc.subject.keywordPlus | BREAST-CANCER | - |
dc.subject.keywordPlus | FACTOR-I | - |
dc.subject.keywordPlus | PATHWAY | - |
dc.subject.keywordPlus | TARGET | - |
dc.subject.keywordPlus | AKT | - |
dc.subject.keywordPlus | CELLS | - |
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