DC Field | Value | Language |
---|---|---|
dc.contributor.author | D Masciocchi | - |
dc.contributor.author | S Villa | - |
dc.contributor.author | F Meneghetti | - |
dc.contributor.author | A Pedretti | - |
dc.contributor.author | D Barlocco | - |
dc.contributor.author | L Legnani | - |
dc.contributor.author | L Toma | - |
dc.contributor.author | Byoung-Mog Kwon | - |
dc.contributor.author | S Nakano | - |
dc.contributor.author | A Asai | - |
dc.contributor.author | A Gelain | - |
dc.date.accessioned | 2017-04-19T09:30:02Z | - |
dc.date.available | 2017-04-19T09:30:02Z | - |
dc.date.issued | 2012 | - |
dc.identifier.issn | 2040-2503 | - |
dc.identifier.uri | 10.1039/c2md20018j | ko |
dc.identifier.uri | https://oak.kribb.re.kr/handle/201005/10709 | - |
dc.description.abstract | Signal 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.publisher | Royal Soc Chemistry | - |
dc.title | 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 | - |
dc.title.alternative | Biological and computational evaluation of an oxadiazole derivative (MD77) as a new lead for direct STAT3 inhibitors | - |
dc.type | Article | - |
dc.citation.title | Medchemcomm | - |
dc.citation.number | 5 | - |
dc.citation.endPage | 599 | - |
dc.citation.startPage | 592 | - |
dc.citation.volume | 3 | - |
dc.contributor.affiliatedAuthor | Byoung-Mog Kwon | - |
dc.contributor.alternativeName | Masciocchi | - |
dc.contributor.alternativeName | Villa | - |
dc.contributor.alternativeName | Meneghetti | - |
dc.contributor.alternativeName | Pedretti | - |
dc.contributor.alternativeName | Barlocco | - |
dc.contributor.alternativeName | Legnani | - |
dc.contributor.alternativeName | Toma | - |
dc.contributor.alternativeName | 권병목 | - |
dc.contributor.alternativeName | Nakano | - |
dc.contributor.alternativeName | Asai | - |
dc.contributor.alternativeName | Gelain | - |
dc.identifier.bibliographicCitation | Medchemcomm, vol. 3, no. 5, pp. 592-599 | - |
dc.identifier.doi | 10.1039/c2md20018j | - |
dc.description.journalClass | N | - |
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