Induction of apoptosis and suppression of angiogenesis of hepatocellular carcinoma by HS-159, a novel phosphatidylinositol 3-kinase inhibitor

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dc.contributor.authorYun, Sun-Miko
dc.contributor.authorLee, Ju-Heeko
dc.contributor.authorJung, Kyung Heeko
dc.contributor.authorLee, Hyunseungko
dc.contributor.authorLee, Soyoungko
dc.contributor.authorHong, Sungwooko
dc.contributor.authorHong, Soon-Sunko
dc.date.accessioned2013-08-14T01:09:20Z-
dc.date.available2013-08-14T01:09:20Z-
dc.date.created2013-08-09-
dc.date.created2013-08-09-
dc.date.issued2013-07-
dc.identifier.citationINTERNATIONAL JOURNAL OF ONCOLOGY, v.43, no.1, pp.201 - 209-
dc.identifier.issn1019-6439-
dc.identifier.urihttp://hdl.handle.net/10203/175026-
dc.description.abstractThe 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.languageEnglish-
dc.publisherSPANDIDOS PUBL LTD-
dc.subjectHYPOXIA-INDUCIBLE FACTOR-1-
dc.subjectENDOTHELIAL GROWTH-FACTOR-
dc.subjectCANCER-THERAPY-
dc.subjectANTITUMOR-ACTIVITY-
dc.subjectBREAST-CANCER-
dc.subjectFACTOR-I-
dc.subjectPATHWAY-
dc.subjectTARGET-
dc.subjectAKT-
dc.subjectCELLS-
dc.titleInduction of apoptosis and suppression of angiogenesis of hepatocellular carcinoma by HS-159, a novel phosphatidylinositol 3-kinase inhibitor-
dc.typeArticle-
dc.identifier.wosid000321023100024-
dc.identifier.scopusid2-s2.0-84879615715-
dc.type.rimsART-
dc.citation.volume43-
dc.citation.issue1-
dc.citation.beginningpage201-
dc.citation.endingpage209-
dc.citation.publicationnameINTERNATIONAL JOURNAL OF ONCOLOGY-
dc.identifier.doi10.3892/ijo.2013.1912-
dc.contributor.localauthorHong, Sungwoo-
dc.contributor.nonIdAuthorYun, Sun-Mi-
dc.contributor.nonIdAuthorLee, Ju-Hee-
dc.contributor.nonIdAuthorJung, Kyung Hee-
dc.contributor.nonIdAuthorLee, Hyunseung-
dc.contributor.nonIdAuthorLee, Soyoung-
dc.contributor.nonIdAuthorHong, Soon-Sun-
dc.type.journalArticleArticle-
dc.subject.keywordAuthorphosphatidylinositol 3-kinase inhibitor-
dc.subject.keywordAuthoranticancer-
dc.subject.keywordAuthorapoptosis-
dc.subject.keywordAuthorangiogenesis-
dc.subject.keywordAuthorhepatocellular carcinoma-
dc.subject.keywordPlusHYPOXIA-INDUCIBLE FACTOR-1-
dc.subject.keywordPlusENDOTHELIAL GROWTH-FACTOR-
dc.subject.keywordPlusCANCER-THERAPY-
dc.subject.keywordPlusANTITUMOR-ACTIVITY-
dc.subject.keywordPlusBREAST-CANCER-
dc.subject.keywordPlusFACTOR-I-
dc.subject.keywordPlusPATHWAY-
dc.subject.keywordPlusTARGET-
dc.subject.keywordPlusAKT-
dc.subject.keywordPlusCELLS-
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