Biological and computational evaluation of an oxadiazole derivative (MD77) as a new lead for direct STAT3 inhibitors = 새로운 STAT3 저해제로 MD77의 생물학적 및 전산학적 평가

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dc.contributor.authorD Masciocchi-
dc.contributor.authorS Villa-
dc.contributor.authorF Meneghetti-
dc.contributor.authorA Pedretti-
dc.contributor.authorD Barlocco-
dc.contributor.authorL Legnani-
dc.contributor.authorL Toma-
dc.contributor.authorByoung-Mog Kwon-
dc.contributor.authorS Nakano-
dc.contributor.authorA Asai-
dc.contributor.authorA Gelain-
dc.date.accessioned2017-04-19T09:30:02Z-
dc.date.available2017-04-19T09:30:02Z-
dc.date.issued2012-
dc.identifier.issn2040-2503-
dc.identifier.uri10.1039/c2md20018jko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/10709-
dc.description.abstractSignal Transducer and Activator of Transcription 3 (STAT3) is a latent cytoplasmic protein overexpressed in various cancer cell lines. STAT3 participates in oncogenesis by stimulating cell proliferation and preventing apoptosis and it has been proven as a suitable target for anticancer therapy. In order to identify direct STAT3 inhibitors, we performed a binding assay on several previously synthesized 1,2,5-oxadiazole derivatives. Among them, compound MD77, N-[4-(4-chlorophenyl)-1,2,5-oxadiazol-3-yl]-4-(trifluoromethyl) benzamide, showed a good ability to bind the STAT3-SH2 domain in a dose-dependent manner (IC 50 = 17.7 μM). Computational studies were carried out to investigate its binding mode. Moreover, compound MD77 showed a significant anti-proliferative activity versus several tumor cell lines. On these bases, compound MD77 was selected as a lead for the future development of direct STAT3 inhibitors.-
dc.publisherRoyal Soc Chemistry-
dc.titleBiological and computational evaluation of an oxadiazole derivative (MD77) as a new lead for direct STAT3 inhibitors = 새로운 STAT3 저해제로 MD77의 생물학적 및 전산학적 평가-
dc.title.alternativeBiological and computational evaluation of an oxadiazole derivative (MD77) as a new lead for direct STAT3 inhibitors-
dc.typeArticle-
dc.citation.titleMedchemcomm-
dc.citation.number5-
dc.citation.endPage599-
dc.citation.startPage592-
dc.citation.volume3-
dc.contributor.affiliatedAuthorByoung-Mog Kwon-
dc.contributor.alternativeNameMasciocchi-
dc.contributor.alternativeNameVilla-
dc.contributor.alternativeNameMeneghetti-
dc.contributor.alternativeNamePedretti-
dc.contributor.alternativeNameBarlocco-
dc.contributor.alternativeNameLegnani-
dc.contributor.alternativeNameToma-
dc.contributor.alternativeName권병목-
dc.contributor.alternativeNameNakano-
dc.contributor.alternativeNameAsai-
dc.contributor.alternativeNameGelain-
dc.identifier.bibliographicCitationMedchemcomm, vol. 3, no. 5, pp. 592-599-
dc.identifier.doi10.1039/c2md20018j-
dc.description.journalClassN-
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