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Identification of a Wells-Dawson polyoxometalatebased AP-2γ inhibitor with pro-apoptotic activity
Hu J.6; Tan S.K.3; Lim M.G.L.3; Chang S.H.6; Cui G.6; Liu S.6; Narasimhan K.3; New S.Y.4; Wang X.1; Chen C.1; Chakravarty H.6; Kolatkar P.R.3; Tam K.Y.6; Lu Q.2; Su X.4; Jauch R.3; Cheung E.6
2018-06-11
Source PublicationBiochemical Journal
ISSN14708728 02646021
Volume475Issue:11Pages:1965-1977
Abstract

AP-2 gamma (AP-2γ) is a transcription factor that plays pivotal roles in breast cancer biology. To search for small molecule inhibitors of AP-2γ, we performed a high-throughput fluorescence anisotropy screen and identified a polyoxometalate compound with Wells-Dawson structure K6[P2Mo18O62] (Dawson-POM) that blocks the DNA-binding activity of AP-2γ. We showed that this blocking activity is due to the direct binding of Dawson-POM to AP-2γ. We also provided evidence to show that Dawson-POM decreases AP-2γ-dependent transcription similar to silencing the gene. Finally, we demonstrated that Dawson-POM contains anti-proliferative and pro-apoptotic effects in breast cancer cells. In summary, we identified the first small molecule inhibitor of AP-2γ and showed Dawson-POM-mediated inhibition of AP-2γ as a potential avenue for cancer therapy.

DOI10.1042/BCJ20170942
URLView the original
Indexed BySCI
Language英语
WOS Research AreaBiochemistry & Molecular Biology
WOS SubjectBiochemistry & Molecular Biology
WOS IDWOS:000436048700006
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Cited Times [WOS]:2   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.Guangzhou Institutes of Biomedicine and Health
2.XuZhou Medical University
3.A-Star, Genome Institute of Singapore
4.A-Star, Institute of Materials Research and Engineering
5.Fujian Agriculture and Forestry University
6.Universidade de Macau
Recommended Citation
GB/T 7714
Hu J.,Tan S.K.,Lim M.G.L.,et al. Identification of a Wells-Dawson polyoxometalatebased AP-2γ inhibitor with pro-apoptotic activity[J]. Biochemical Journal,2018,475(11):1965-1977.
APA Hu J..,Tan S.K..,Lim M.G.L..,Chang S.H..,Cui G..,...&Cheung E..(2018).Identification of a Wells-Dawson polyoxometalatebased AP-2γ inhibitor with pro-apoptotic activity.Biochemical Journal,475(11),1965-1977.
MLA Hu J.,et al."Identification of a Wells-Dawson polyoxometalatebased AP-2γ inhibitor with pro-apoptotic activity".Biochemical Journal 475.11(2018):1965-1977.
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