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Your search keyword '"Edwin, Cheung"' showing total 2 results
Start Over Author "Edwin, Cheung" Publisher portland press ltd.
2 results on '"Edwin, Cheung"'

1. DNA-binding activity of the transcription factor upstream stimulatory factor 1 (USF-1) is regulated by cyclin-dependent phosphorylation

Author

Edwin Cheung, Petra S.M. Mayr, Federico Coda-Zabetta, Phillip G. Woodman, and David S.W. Boam

Subjects
Cyclin-dependent kinase 1, biology, Cyclin D, Cyclin A, USF2, Cell Biology, Biochemistry, Molecular biology, Upstream Stimulatory Factor, Sp3 transcription factor, biology.protein, Cyclin B1, Molecular Biology, Cyclin A2
Abstract

The ubiquitous transcription factor upstream stimulatory factor (USF) 1 is a member of the bzHLH (leucine zipper-basic-helix-loop-helix) family, which is structurally related to the Myc family of proteins. It plays a role in the regulation of many genes, including the cyclin B1 gene, which is active during the G2/M and M phases of the cell cycle and may also play a role in the regulation of cellular proliferation. We show that the affinity of recombinant USF-1 for DNA is greatly increased by treatment with active cyclin A2-p34cdc2 or cyclin B1-p34cdc2 complexes and that its interaction with DNA is dependent on p34cdc2-mediated phosphorylation. We have localized the phosphorylation site(s) to a region that lies outside the minimal DNA-binding domain but overlaps with the previously identified USF-specific region. Deletion studies of USF-1 suggest that amino acids 143-197 regulate DNA-binding activity in a phosphorylation-dependent manner.

Published
1999
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2. Identification of a Wells-Dawson polyoxometalate-based AP-2γ inhibitor with pro-apoptotic activity.

Author

Jiamiao Hu, Si Kee Tan, Michelle Gek Liang Lim, Shie Hong Chang, Guimei Cui, Shanshan Liu, Narasimhan, Kamesh, Siu Yee New, Xuecong Wang, Congling Chen, Chakravarty, Harapriya, Kolatkar, Prasanna R., Kin Yip Tam, Qian Lu, Xiaodi Su, Jauch, Ralf, and Edwin Cheung

Subjects
TRANSCRIPTION factors, BREAST cancer, DNA-binding proteins, SMALL molecules, CANCER treatment
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. [ABSTRACT FROM AUTHOR]

Published
2018
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