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Exploring the formation and recognition of an important G-quadruplex in a HIF1α promoter and its transcriptional inhibition by a benzo [c] phenanthridine derivative

H Chen, H Long, X Cui, J Zhou, M Xu…

文献索引:Chen, Han; Long, Haitao; Cui, Xiaojie; Zhou, Jiang; Xu, Ming; Yuan, Gu Journal of the American Chemical Society, 2014 , vol. 136, # 6 p. 2583 - 2591

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被引用次数: 20

摘要

Four putative G-quadruplex sequences (PGSs) in the HIF1α promoter and the 5′ UTR were evaluated for their G-quadruplex-forming potential using ESI-MS, CD, FRET, DMS footprinting, and a polymerase stop assay. An important G-quadruplex (S1) has been proven to inhibit HIF1α transcription by blocking AP2 binding. A benzo [c] phenanthridine derivative was found to target the S1 G-quadruplex and induce its conformational conversion from ...