UM
Anticancer osmium complex inhibitors of the HIF-1α and p300 protein-protein interaction
Yang C.; Wang W.; Li G.-D.; Zhong H.-J.; Dong Z.-Z.; Wong C.-Y.; Kwong D.W.J.; Ma D.-L.; Leung C.-H.
2017
Source PublicationScientific Reports
ISSN20452322
Volume7
AbstractThe hypoxia inducible factor (HIF) pathway has been considered to be an attractive anti-cancer target. One strategy to inhibit HIF activity is through the disruption of the HIF-1α-p300 protein-protein interaction. We report herein the identification of an osmium(II) complex as the first metal-based inhibitor of the HIF-1α-p300 interaction. We evaluated the effect of complex 1 on HIF-1α signaling pathway in vitro and in cellulo by using the dual luciferase reporter assay, co-immunoprecipitation assay, and immunoblot assay. Complex 1 exhibited a dose-dependent inhibition of HRE-driven luciferase activity, with an IC 50 value of 1.22 μM. Complex 1 interfered with the HIF-1α-p300 interaction as revealed by a dose-dependent reduction of p300 co-precipitated with HIF-1α as the concentration of complex 1 was increased. Complex 1 repressed the phosphorylation of SRC, AKT and STAT3, and had no discernible effect on the activity of NF-k B. We anticipate that complex 1 could be utilized as a promising scaffold for the further development of more potent HIF-1α inhibitors for anti-cancer treatment. © The Author(s) 2017.
DOI10.1038/srep42860
URLView the original
Language英语
The Source to ArticleScopus
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Cited Times [WOS]:11   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
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GB/T 7714
Yang C.,Wang W.,Li G.-D.,et al. Anticancer osmium complex inhibitors of the HIF-1α and p300 protein-protein interaction[J]. Scientific Reports,2017,7.
APA Yang C..,Wang W..,Li G.-D..,Zhong H.-J..,Dong Z.-Z..,...&Leung C.-H..(2017).Anticancer osmium complex inhibitors of the HIF-1α and p300 protein-protein interaction.Scientific Reports,7.
MLA Yang C.,et al."Anticancer osmium complex inhibitors of the HIF-1α and p300 protein-protein interaction".Scientific Reports 7(2017).
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