DC Field | Value | Language |
---|---|---|
dc.contributor.author | Yun, Sun-Mi | ko |
dc.contributor.author | Jung, Kyung Hee | ko |
dc.contributor.author | Kim, Soo Jung | ko |
dc.contributor.author | Fang, Zhenghuan | ko |
dc.contributor.author | Son, Mi Kwon | ko |
dc.contributor.author | Yan, Hong Hua | ko |
dc.contributor.author | Lee, Hyunseung | ko |
dc.contributor.author | Kim, JinHee | ko |
dc.contributor.author | Shin, Sanghye | ko |
dc.contributor.author | Hong, Sungwoo | ko |
dc.contributor.author | Hong, Soon-Sun | ko |
dc.date.accessioned | 2014-09-01T08:38:53Z | - |
dc.date.available | 2014-09-01T08:38:53Z | - |
dc.date.created | 2014-07-07 | - |
dc.date.created | 2014-07-07 | - |
dc.date.issued | 2014-06 | - |
dc.identifier.citation | CANCER LETTERS, v.348, no.1-2, pp.50 - 60 | - |
dc.identifier.issn | 0304-3835 | - |
dc.identifier.uri | http://hdl.handle.net/10203/189634 | - |
dc.description.abstract | Imatinib 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.language | English | - |
dc.publisher | ELSEVIER IRELAND LTD | - |
dc.subject | CELL-DEATH | - |
dc.subject | CANCER-THERAPY | - |
dc.subject | TYROSINE KINASE | - |
dc.subject | CDK INHIBITORS | - |
dc.subject | MECHANISMS | - |
dc.subject | MUTANT | - |
dc.subject | APOPTOSIS | - |
dc.subject | PROTEINS | - |
dc.subject | GLEEVEC | - |
dc.subject | VX-680 | - |
dc.title | HS-438, a new inhibitor of Imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia | - |
dc.type | Article | - |
dc.identifier.wosid | 000336878100006 | - |
dc.identifier.scopusid | 2-s2.0-84900466184 | - |
dc.type.rims | ART | - |
dc.citation.volume | 348 | - |
dc.citation.issue | 1-2 | - |
dc.citation.beginningpage | 50 | - |
dc.citation.endingpage | 60 | - |
dc.citation.publicationname | CANCER LETTERS | - |
dc.identifier.doi | 10.1016/j.canlet.2014.03.012 | - |
dc.embargo.liftdate | 9999-12-31 | - |
dc.embargo.terms | 9999-12-31 | - |
dc.contributor.localauthor | Hong, Sungwoo | - |
dc.contributor.nonIdAuthor | Yun, Sun-Mi | - |
dc.contributor.nonIdAuthor | Jung, Kyung Hee | - |
dc.contributor.nonIdAuthor | Kim, Soo Jung | - |
dc.contributor.nonIdAuthor | Fang, Zhenghuan | - |
dc.contributor.nonIdAuthor | Son, Mi Kwon | - |
dc.contributor.nonIdAuthor | Yan, Hong Hua | - |
dc.contributor.nonIdAuthor | Lee, Hyunseung | - |
dc.contributor.nonIdAuthor | Hong, Soon-Sun | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | HS-438 | - |
dc.subject.keywordAuthor | BCR-ABL | - |
dc.subject.keywordAuthor | T315I | - |
dc.subject.keywordAuthor | Chronic myeloid leukemia | - |
dc.subject.keywordPlus | CELL-DEATH | - |
dc.subject.keywordPlus | CANCER-THERAPY | - |
dc.subject.keywordPlus | TYROSINE KINASE | - |
dc.subject.keywordPlus | CDK INHIBITORS | - |
dc.subject.keywordPlus | MECHANISMS | - |
dc.subject.keywordPlus | MUTANT | - |
dc.subject.keywordPlus | APOPTOSIS | - |
dc.subject.keywordPlus | PROTEINS | - |
dc.subject.keywordPlus | GLEEVEC | - |
dc.subject.keywordPlus | VX-680 | - |
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