CSpace  > 2018期刊论文
Identification of a Wells-Dawson polyoxometalate-based AP-2 gamma inhibitor with pro-apoptotic activity
Hu, Jiamiao; Tan, Si Kee; Lim, Michelle Gek Liang; Chang, Shie Hong; Cui, Guimei; Liu, Shanshan; Narasimhan, Kamesh; New, Siu Yee; Wang, Xuecong; Chen, Congling; Chakravarty, Harapriya; Kolatkar, Prasanna R.; Tam, Kin Yip; Lu, Qian; Su, Xiaodi; Jauch, Ralf; Cheung, Edwin
2019-06-15
Source PublicationBIOCHEMICAL JOURNAL
Volume475Pages:1965-1977
AbstractAP-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.
Indexed BySCIE
Document Type期刊论文
Identifierhttp://ir.foo.ac.cn/handle/2SETSVCV/1469
Collection2018期刊论文
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,2019,475:1965-1977.
APA Hu, Jiamiao.,Tan, Si Kee.,Lim, Michelle Gek Liang.,Chang, Shie Hong.,Cui, Guimei.,...&Cheung, Edwin.(2019).Identification of a Wells-Dawson polyoxometalate-based AP-2 gamma inhibitor with pro-apoptotic activity.BIOCHEMICAL JOURNAL,475,1965-1977.
MLA Hu, Jiamiao,et al."Identification of a Wells-Dawson polyoxometalate-based AP-2 gamma inhibitor with pro-apoptotic activity".BIOCHEMICAL JOURNAL 475(2019):1965-1977.
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