A cyclometallated iridium(III) complex as a c-myc G-Quadruplex stabilizer and down-regulator of c-myc oncogene expression

H. Yang, V. P.Y. Ma, D. S.H. Chan, H. Z. He, C. H. Leung, Edmond Dik Lung MA*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

16 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)576-582
Number of pages7
JournalCurrent Medicinal Chemistry
Volume20
Issue number4
DOIs
Publication statusPublished - Feb 2013

Scopus Subject Areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

User-Defined Keywords

  • C-myc
  • DNA
  • G-quadruplex
  • Iridium(III)
  • Metal complex
  • Oncogene
  • Promoter

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