HS-438, a new inhibitor of Imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia

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dc.contributor.authorYun, Sun-Miko
dc.contributor.authorJung, Kyung Heeko
dc.contributor.authorKim, Soo Jungko
dc.contributor.authorFang, Zhenghuanko
dc.contributor.authorSon, Mi Kwonko
dc.contributor.authorYan, Hong Huako
dc.contributor.authorLee, Hyunseungko
dc.contributor.authorKim, JinHeeko
dc.contributor.authorShin, Sanghyeko
dc.contributor.authorHong, Sungwooko
dc.contributor.authorHong, Soon-Sunko
dc.date.accessioned2014-09-01T08:38:53Z-
dc.date.available2014-09-01T08:38:53Z-
dc.date.created2014-07-07-
dc.date.created2014-07-07-
dc.date.issued2014-06-
dc.identifier.citationCANCER LETTERS, v.348, no.1-2, pp.50 - 60-
dc.identifier.issn0304-3835-
dc.identifier.urihttp://hdl.handle.net/10203/189634-
dc.description.abstractImatinib is a selective breakpoint cluster region-Abelson (BCR-ABL) tyrosine kinase inhibitor (TKI) that has significantly improved the prognosis of patients with chronic myeloid leukemia (CML). However, T315I gene mutations of the BCR-ABL kinase domain have been shown to confer resistance to Imatinib. In the present study, we synthesized a novel BCR-ABL inhibitor, HS-438, and identified its anti-leukemic effects in vitro and in vivo. We found that HS-438 strongly inhibited the expression of BCR-ABL signaling pathways in wild-type BCR-ABL (BaF3/WT) cells as well as T315I-mutated BCR-ABL (BaF3/T315I) cells with resistance to Imatinib. HS-438 induced cell cycle arrest, particularly during the G(0)/G(1), cell cycle phase, and induced apoptosis. In BaF3/T315I xenograft models, HS-438 significantly delayed tumor growth, unlike Imatinib. In summary, we suggest that HS-438 may be a novel drug candidate with the therapeutic potential to target BCR-ABL and overcome Imatinib resistance in patients with CML.-
dc.languageEnglish-
dc.publisherELSEVIER IRELAND LTD-
dc.subjectCELL-DEATH-
dc.subjectCANCER-THERAPY-
dc.subjectTYROSINE KINASE-
dc.subjectCDK INHIBITORS-
dc.subjectMECHANISMS-
dc.subjectMUTANT-
dc.subjectAPOPTOSIS-
dc.subjectPROTEINS-
dc.subjectGLEEVEC-
dc.subjectVX-680-
dc.titleHS-438, a new inhibitor of Imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia-
dc.typeArticle-
dc.identifier.wosid000336878100006-
dc.identifier.scopusid2-s2.0-84900466184-
dc.type.rimsART-
dc.citation.volume348-
dc.citation.issue1-2-
dc.citation.beginningpage50-
dc.citation.endingpage60-
dc.citation.publicationnameCANCER LETTERS-
dc.identifier.doi10.1016/j.canlet.2014.03.012-
dc.embargo.liftdate9999-12-31-
dc.embargo.terms9999-12-31-
dc.contributor.localauthorHong, Sungwoo-
dc.contributor.nonIdAuthorYun, Sun-Mi-
dc.contributor.nonIdAuthorJung, Kyung Hee-
dc.contributor.nonIdAuthorKim, Soo Jung-
dc.contributor.nonIdAuthorFang, Zhenghuan-
dc.contributor.nonIdAuthorSon, Mi Kwon-
dc.contributor.nonIdAuthorYan, Hong Hua-
dc.contributor.nonIdAuthorLee, Hyunseung-
dc.contributor.nonIdAuthorHong, Soon-Sun-
dc.type.journalArticleArticle-
dc.subject.keywordAuthorHS-438-
dc.subject.keywordAuthorBCR-ABL-
dc.subject.keywordAuthorT315I-
dc.subject.keywordAuthorChronic myeloid leukemia-
dc.subject.keywordPlusCELL-DEATH-
dc.subject.keywordPlusCANCER-THERAPY-
dc.subject.keywordPlusTYROSINE KINASE-
dc.subject.keywordPlusCDK INHIBITORS-
dc.subject.keywordPlusMECHANISMS-
dc.subject.keywordPlusMUTANT-
dc.subject.keywordPlusAPOPTOSIS-
dc.subject.keywordPlusPROTEINS-
dc.subject.keywordPlusGLEEVEC-
dc.subject.keywordPlusVX-680-
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