1. Academic Validation
  2. Inhibition of cell proliferation by quindoline derivative (SYUIQ-05) through its preferential interaction with c-myc promoter G-quadruplex

Inhibition of cell proliferation by quindoline derivative (SYUIQ-05) through its preferential interaction with c-myc promoter G-quadruplex

  • J Med Chem. 2011 Aug 25;54(16):5671-9. doi: 10.1021/jm200062u.
Tian-Miao Ou 1 Jing Lin Yu-Jing Lu Jin-Qiang Hou Jia-Heng Tan Shu-Han Chen Zeng Li Yan-Ping Li Ding Li Lian-Quan Gu Zhi-Shu Huang
Affiliations

Affiliation

  • 1 School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou University City, Waihuan East Road 132, Guangzhou 510006, People's Republic of China.
Abstract

G-quadruplex is a special DNA secondary structure and present in many important regulatory regions in human genome, such as the telomeric end and the promoters of some oncogenes. Specially, different forms of G-quadruplexes exist in telomeric DNA and c-Myc promoter and play important roles in the pathway of cell proliferation and senescence. The effects of G-quadruplex ligands for either telomeric or c-myc G-quadruplex in vitro have been widely studied, but the specificity of these effects in vivo is still unknown. In the present research, various experiments were carried out to study the effect of G-quadruplex ligand SYUIQ-05 on tumor cell lines and the mechanism of this effect. Our results showed that it preferred to bind with G-quadruplex in c-Myc and had rather insignificant effect on G-quadruplex in telomere. Therefore, it is possible that this compound had its antitumor activity for Cancer cells mainly through its interaction with c-Myc quadruplex.

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