A Cyclometallated Iridium(III) Complex As a c-myc G-Quadruplex Stabilizer and Down-Regulator of c-myc Oncogene Expression

被引:0
作者
Yang, H. [1 ]
Ma, V. P. -Y. [1 ]
Chan, D. S. -H. [1 ]
He, H. -Z. [1 ]
Leung, C. -H. [2 ]
Ma, D. -L. [1 ]
机构
[1] Hong Kong Baptist Univ, Dept Chem, Kowloon Tong, Hong Kong, Peoples R China
[2] Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Taipa, Peoples R China
关键词
c-myc; DNA; G-quadruplex; iridium(III); metal complex; oncogene; promoter; NUCLEASE-HYPERSENSITIVE ELEMENT; METAL-COMPLEXES; TELOMERASE ACTIVITY; DNA; PROMOTER; BINDING; RECOGNITION; INHIBITION; PROBES; SQUARE;
D O I
暂无
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A new cyclometallated iridium(III) complex with the 2,2'-biquinoline N-donor ligand has been synthesized and characterized. The interaction and affinity of the complex towards c-myc G-quadruplex and duplex DNA have been investigated using UV/Vis spectroscopy and gel mobility shift assay. These studies revealed that complex 1 binds to c-myc G-quadruplexes (Pu22 and Pu27) with high affinity but does not interact with duplex DNA either by intercalation or groove binding. The ability of 1 to stabilize c-myc G-quadruplex DNA in vitro has also been examined through a PCR stop assay and a cell-based luciferase reporter assay. Complex 1 displays promising cytotoxic activity against the HeLa cell line with sub-micromolar potency.
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页码:576 / 582
页数:7
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