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Identification of a Wells-Dawson polyoxometalate-based AP-2 gamma inhibitor with pro-apoptotic activity
Hu, Jiamiao1,2; Tan, Si Kee3; Lim, Michelle Gek Liang3; Chang, Shie Hong1; Cui, Guimei1; Liu, Shanshan1,4; Narasimhan, Kamesh3; New, Siu Yee5; Wang, Xuecong6; Chen, Congling6; Chakravarty, Harapriya1; Kolatkar, Prasanna R.3; Tam, Kin Yip1; Lu, Qian4; Su, Xiaodi5; Jauch, Ralf3,6; Cheung, Edwin1,3
2018-06-15
Source PublicationBIOCHEMICAL JOURNAL
ISSN0264-6021
Volume475Issue:11Pages:1965-1977
Abstract

AP-2 gamma (AP-2 gamma) is a transcription factor that plays pivotal roles in breast cancer biology. To search for small molecule inhibitors of AP-2 gamma, we performed a high-throughput fluorescence anisotropy screen and identified a polyoxometalate compound with Wells-Dawson structure K-6[P2Mo18O62] (Dawson-POM) that blocks the DNA-binding activity of AP-2 gamma. We showed that this blocking activity is due to the direct binding of Dawson-POM to AP-2 gamma. We also provided evidence to show that Dawson-POM decreases AP-2 gamma-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-2 gamma and showed Dawson-POM-mediated inhibition of AP-2 gamma as a potential avenue for cancer therapy.

KeywordAp-2γ Breast Cancer Fluorescent Anisotropic Polyoxometalate
DOIhttp://doi.org/10.1042/BCJ20170942
URLView the original
Indexed BySCI
Language英语
WOS Research AreaBiochemistry & Molecular Biology
WOS SubjectBiochemistry & Molecular Biology
WOS IDWOS:000436048700006
PublisherPORTLAND PRESS LTD
The Source to ArticleWOS
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Cited Times [WOS]:2   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.Faculty of Health Sciences, University of Macau, Macau, China
2.College of Food Science, Fujian Agriculture and Forestry University, Fuzhou, Fujian, China.
3.Genome Institute of Singapore, A*STAR (Agency for Science, Technology, and Research), Singapore.
4.Xuzhou Medical University, Xuzhou, Jiangsu, China.
5.Institute of Materials Research and Engineering, A*STAR, Singapore.
6.Guangzhou Institute of Biomedicine and Health, Guangzhou, Guangdong, China.
First Author AffilicationFaculty of Health Sciences
Recommended Citation
GB/T 7714
Hu, Jiamiao,Tan, Si Kee,Lim, Michelle Gek Liang,et al. Identification of a Wells-Dawson polyoxometalate-based AP-2 gamma inhibitor with pro-apoptotic activity[J]. BIOCHEMICAL JOURNAL,2018,475(11):1965-1977.
APA Hu, Jiamiao.,Tan, Si Kee.,Lim, Michelle Gek Liang.,Chang, Shie Hong.,Cui, Guimei.,...&Cheung, Edwin.(2018).Identification of a Wells-Dawson polyoxometalate-based AP-2 gamma inhibitor with pro-apoptotic activity.BIOCHEMICAL JOURNAL,475(11),1965-1977.
MLA Hu, Jiamiao,et al."Identification of a Wells-Dawson polyoxometalate-based AP-2 gamma inhibitor with pro-apoptotic activity".BIOCHEMICAL JOURNAL 475.11(2018):1965-1977.
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