Turning off transcription of the bcl-2 gene by stabilizing the bcl-2 promoter quadruplex with quindoline derivatives.

@article{Wang2010TurningOT,
  title={Turning off transcription of the bcl-2 gene by stabilizing the bcl-2 promoter quadruplex with quindoline derivatives.},
  author={Xiaodong Wang and Tian-Miao Ou and Yu-jing Lu and Zeng Li and Zheng Xu and Chen Xi and Jia-Heng Tan and Shi-Liang Huang and Lin-kun An and Ding Yang Li and Lian-Quan Gu and Zhi-Shu Huang},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 11},
  pages={4390-8}
}
Human bcl-2 gene is an apoptosis-related oncogene containing a GC-rich sequence which is located upstream from P1 promoter and has the potential to form G-quadruplex structures. However, the regulatory role of the quadruplex and the effect of its ligands on bcl-2 have not been clarified. Here, we demonstrated that the G-quadruplex structure was disrupted when partial mutation of G --> A was made, resulting in a 2-fold increase in basal transcriptional activity of bcl-2 promoter. Quindoline… CONTINUE READING

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