title: A cyclometallated iridium(III) complex as a c-myc G-quadruplex stabilizer and down-regulator of c-myc oncogene expression.
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.
authors.affiliation: Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China.
authors.forename: H
authors.initials: H
authors.lastname: Yang
authors.forename: V P-Y
authors.initials: VP
authors.lastname: Ma
authors.forename: D S-H
authors.initials: DS
authors.lastname: Chan
authors.forename: H-Z
authors.initials: HZ
authors.lastname: He
authors.forename: C-H
authors.initials: CH
authors.lastname: Leung
authors.forename: D-L
authors.initials: DL
authors.lastname: Ma
mesh_terms: D056831:Coordination Complexes / Q000737:chemistry* / Q000494:pharmacology; D015536:Down-Regulation; D054856:G-Quadruplexes; D016259:Genes, myc / Q000187:drug effects*; D006367:HeLa Cells; D006801:Humans; D007495:Iridium / Q000737:chemistry*; D008958:Models, Molecular; D016271:Proto-Oncogene Proteins c-myc / Q000096:biosynthesis* / Q000235:genetics / Q000378:metabolism; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology; D013056:Spectrophotometry, Ultraviolet
chemical_list: D056831:Coordination Complexes; D016271:Proto-Oncogene Proteins c-myc; D011804:Quinolines; D007495:Iridium