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Cited 31 times in

EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis.

DC FieldValueLanguage
dc.contributor.author김승원-
dc.date.accessioned2015-12-28T11:07:31Z-
dc.date.available2015-12-28T11:07:31Z-
dc.date.issued2014-
dc.identifier.issn1535-7163-
dc.identifier.urihttps://ir.ymlib.yonsei.ac.kr/handle/22282913/138745-
dc.description.abstractAdvanced tumors produce an excessive amount of transforming growth factor β (TGFβ), which promotes tumor progression at late stages of malignancy. The purpose of this study was to develop anti-TGFβ therapeutics for cancer. We synthesized a novel small-molecule TGFβ receptor I kinase (activin receptor-like kinase 5) inhibitor termed N-[[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl]methyl]-2-fluoroaniline (EW-7197), and we investigated its potential antimetastatic efficacy in mouse mammary tumor virus (MMTV)/c-Neu mice and 4T1 orthotopic-grafted mice. EW-7197 inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice and 4T1 orthotopic-grafted mice. EW-7197 also inhibited the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Furthermore, EW-7197 enhanced cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice. In summary, EW-7197 showed potent in vivo antimetastatic activity, indicating its potential for use as an anticancer therapy.-
dc.description.statementOfResponsibilityopen-
dc.format.extent1704~1716-
dc.relation.isPartOfMolecular Cancer Therapeutics-
dc.rightsCC BY-NC-ND 2.0 KR-
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/2.0/kr/-
dc.subject.MESHAniline Compounds/pharmacology*-
dc.subject.MESHAnimals-
dc.subject.MESHBreast Neoplasms/drug therapy*-
dc.subject.MESHBreast Neoplasms/enzymology-
dc.subject.MESHBreast Neoplasms/pathology*-
dc.subject.MESHCell Line, Tumor-
dc.subject.MESHFemale-
dc.subject.MESHHumans-
dc.subject.MESHLung Neoplasms/enzymology-
dc.subject.MESHLung Neoplasms/prevention & control*-
dc.subject.MESHLung Neoplasms/secondary*-
dc.subject.MESHMice-
dc.subject.MESHMice, Inbred BALB C-
dc.subject.MESHProtein Kinase Inhibitors/pharmacology*-
dc.subject.MESHProtein-Serine-Threonine Kinases/antagonists & inhibitors*-
dc.subject.MESHRandom Allocation-
dc.subject.MESHReceptors, Transforming Growth Factor beta/antagonists & inhibitors*-
dc.subject.MESHSignal Transduction/drug effects-
dc.subject.MESHTriazoles/pharmacology*-
dc.subject.MESHXenograft Model Antitumor Assays-
dc.titleEW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis.-
dc.typeArticle-
dc.contributor.collegeCollege of Medicine (의과대학)-
dc.contributor.departmentDept. of Life Science (의생명과학부)-
dc.contributor.googleauthorJi Yeon Son-
dc.contributor.googleauthorSo Yeon Park-
dc.contributor.googleauthorSol Ji Kim-
dc.contributor.googleauthorSeon Joo Lee-
dc.contributor.googleauthorSang A. Park-
dc.contributor.googleauthorMin Jin Kim-
dc.contributor.googleauthorSeung Won Kim-
dc.contributor.googleauthorDae Kee Kim-
dc.contributor.googleauthorJeong Seok Nam-
dc.contributor.googleauthorYhun Yhong Sheen-
dc.identifier.doi10.1158/1535-7163.MCT-13-0903-
dc.admin.authorfalse-
dc.admin.mappingfalse-
dc.contributor.localIdA00656-
dc.relation.journalcodeJ02254-
dc.identifier.pmid24817629-
dc.contributor.alternativeNameKim, Seung Won-
dc.contributor.affiliatedAuthorKim, Seung Won-
dc.citation.volume13-
dc.citation.number7-
dc.citation.startPage1704-
dc.citation.endPage1716-
dc.identifier.bibliographicCitationMolecular Cancer Therapeutics, Vol.13(7) : 1704-1716, 2014-
Appears in Collections:
1. College of Medicine (의과대학) > BioMedical Science Institute (의생명과학부) > 1. Journal Papers

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