Mr. Bo-Xin Zheng


Target-specific fluorescent probes that selectively bind to biologically important macromolecules, such as lipids, proteins, carbohydrates, and nucleic acids with special structures, can offer a powerful molecular tool for real-time study of their subcellular localization and dynamics of these biomolecules with advanced microscopy techniques1-4. DNA G4-structures from human c-MYC promoter is considered as important drug targets5-9; however, the developing of small-molecule-based fluorescent binding ligands that are highly selective targeting these G4-structures over other types of nucleic acids is challenging10-12. Herein, a small-sized c-MYC promoter G-quadruplex selective fluorescent BZT-Indolium binding ligand was demonstrated for the first time as a highly target-specific and photostable probe for in vitro staining and live cell imaging and it was found to be able to inhibit the amplification of the c-MYC G-rich sequence (G-quadruplex) and down-regulate oncogene c-MYC expression in HeLa cancer cells.


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  2. Zhang, S. G.; Sun, H. X.; Wang, L. X.; Liu, Y.; Chen, H. B.; Li, Q.; Guan, A. J.; Liu, M. R.; Tang, Y. L. Nucleic Acids Research, 2018, 46, 7522 – 7532.
  3. Umar, M. I.; Ji, D.; Chan, C. Y.; Kwok, C. K. Molecules, 2019, 24, 2416.
  4. Monchaud, D. Annual Reports in Medicinal Chemistry, 2020, 54, 133.
  5. Brooks, T. A.; Hurley, L. H. Nature Reviews Cancer, 2009, 9, 849-861.
  6. Schmidt, E. V. Oncogene, 1999, 18, 2988 – 2996.
  7. Miller, D. M.; Thomas, S. D.; Islam, A.; Muench, D.; Sedoris, K. Clinical Cancer Research, 2012, 18, 5546 – 5553.
  8. Dang, C. V. Cell, 2012, 149, 22 -35.
  9. Ritapa, C.; Semantee, B.; Jyotirmayee, D.; Santanu. B. Journal of Medicinal Chemistry, 2021, 64, 42 – 70.
  10. Zhai, Q.; Gao, C.; Ding, J.; Zhang, Y.; Islam, B.; Lan, W.; Hou, H.; Deng, H.; Li, J.; Hu, Z. Nucleic Acids Research, 2019, 47, 2190 – 2204.
  11. Hu, M. H.; Wang, Y. Q.; Yu, Z. Y.; Hu, L. N.; Tan, J. H. Journal of Medicinal Chemistry, 2018, 61, 2447 – 2459.
  12. Wang, K. B.; Elsayed, M. S. A.; Wu, G.; Deng, N.; Cushman, M.; Yang, D. Journal of the American Chemical Society, 2019, 141, 11059 – 11070. 

University: PolyU

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