A novel pyruvate kinase M2 activator compound that suppresses lung cancer cell viability under hypoxia = 저산소 상태에서 폐암 생장을 억제하는 신규 피루베이트 카이네이즈 M2 활성물질

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dc.contributor.authorDong Joon Kim-
dc.contributor.authorYoung Soo Park-
dc.contributor.authorN D Kim-
dc.contributor.authorS H Min-
dc.contributor.authorYeon Mi You-
dc.contributor.authorYuri Jung-
dc.contributor.authorHan Koo-
dc.contributor.authorHanmi Noh-
dc.contributor.authorJung Ae Kim-
dc.contributor.authorKyung Chan Park-
dc.contributor.authorYoung Il Yeom-
dc.date.accessioned2017-04-19T10:03:26Z-
dc.date.available2017-04-19T10:03:26Z-
dc.date.issued2015-
dc.identifier.issn1016-8478-
dc.identifier.uri10.14348/molcells.2015.2314ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/12575-
dc.description.abstractPyruvate kinase M2 isoform (PKM2), a rate-limiting enzyme in the final step of glycolysis, is known to be associated with the metabolic rewiring of cancer cells, and considered an important cancer therapeutic target. Herein, we report a novel PKM2 activator, PA-12, which was identified via the molecular docking-based virtual screening. We demonstrate that PA-12 stimulates the pyruvate kinase activity of recombinant PKM2 in vitro, with a half-maximal activity concentration of 4.92 μM, and effectively suppresses both anchorage-dependent and -independent growth of lung cancer cells in non-essential amino acid-depleted medium. In addition, PA-12 blocked the nuclear translocalization of PKM2 in lung cancer cells, resulting in the inhibition of hypoxia response element (HRE)-mediated reporter activity as well as hypoxia-inducible factor 1 (HIF-1) target gene expression, eventually leading to the suppression of cell viability under hypoxia. We also verified that the effects of PA-12 were dependent on PKM2 expression in cancer cells, demonstrating the specificity of PA-12 for PKM2 protein. Taken together, our data suggest that PA-12 is a novel and potent PKM2 activator that has therapeutic implications for lung cancer.-
dc.publisherKorea Soc-Assoc-Inst-
dc.titleA novel pyruvate kinase M2 activator compound that suppresses lung cancer cell viability under hypoxia = 저산소 상태에서 폐암 생장을 억제하는 신규 피루베이트 카이네이즈 M2 활성물질-
dc.title.alternativeA novel pyruvate kinase M2 activator compound that suppresses lung cancer cell viability under hypoxia-
dc.typeArticle-
dc.citation.titleMolecules and Cells-
dc.citation.number4-
dc.citation.endPage379-
dc.citation.startPage373-
dc.citation.volume38-
dc.contributor.affiliatedAuthorDong Joon Kim-
dc.contributor.affiliatedAuthorYoung Soo Park-
dc.contributor.affiliatedAuthorYeon Mi You-
dc.contributor.affiliatedAuthorYuri Jung-
dc.contributor.affiliatedAuthorHan Koo-
dc.contributor.affiliatedAuthorHanmi Noh-
dc.contributor.affiliatedAuthorJung Ae Kim-
dc.contributor.affiliatedAuthorKyung Chan Park-
dc.contributor.affiliatedAuthorYoung Il Yeom-
dc.contributor.alternativeName김동준-
dc.contributor.alternativeName박영수-
dc.contributor.alternativeName김남두-
dc.contributor.alternativeName민상현-
dc.contributor.alternativeName유연미-
dc.contributor.alternativeName정유리-
dc.contributor.alternativeName구한-
dc.contributor.alternativeName노한미-
dc.contributor.alternativeName김정애-
dc.contributor.alternativeName박경찬-
dc.contributor.alternativeName염영일-
dc.identifier.bibliographicCitationMolecules and Cells, vol. 38, no. 4, pp. 373-379-
dc.identifier.doi10.14348/molcells.2015.2314-
dc.subject.keywordhypoxia-
dc.subject.keywordlung cancer-
dc.subject.keywordPA-12-
dc.subject.keywordPKM2 activator-
dc.subject.localhypoxia-
dc.subject.localHypoxia-
dc.subject.locallung cancer-
dc.subject.localLung Cancer-
dc.subject.localLung cancer-
dc.subject.localPA-12-
dc.subject.localPKM2 activator-
dc.description.journalClassY-
Appears in Collections:
Aging Convergence Research Center > 1. Journal Articles
Division of Biomedical Research > Personalized Genomic Medicine Research Center > 1. Journal Articles
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