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; D. L. Ma

doi:10.2174/092986713804910175

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, D. L. Ma^*

^*Corresponding author for this work

Department of Chemistry

Research output: Contribution to journal › Journal article › peer-review

18 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 language	English
Pages (from-to)	576-582
Number of pages	7
Journal	Current Medicinal Chemistry
Volume	20
Issue number	4
DOIs	https://doi.org/10.2174/092986713804910175
Publication status	Published - 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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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.",

keywords = "C-myc, DNA, G-quadruplex, Iridium(III), Metal complex, Oncogene, Promoter",

author = "H. Yang and Ma, {V. P.Y.} and Chan, {D. S.H.} and He, {H. Z.} and Leung, {C. H.} and Ma, {D. L.}",

year = "2013",

month = feb,

doi = "10.2174/092986713804910175",

language = "English",

volume = "20",

pages = "576--582",

journal = "Current Medicinal Chemistry",

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T1 - A cyclometallated iridium(III) complex as a c-myc G-Quadruplex stabilizer and down-regulator of c-myc oncogene expression

AU - Yang, H.

AU - Ma, V. P.Y.

AU - Chan, D. S.H.

AU - He, H. Z.

AU - Leung, C. H.

AU - Ma, D. L.

PY - 2013/2

Y1 - 2013/2

N2 - 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.

AB - 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.

KW - C-myc

KW - DNA

KW - G-quadruplex

KW - Iridium(III)

KW - Metal complex

KW - Oncogene

KW - Promoter

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U2 - 10.2174/092986713804910175

DO - 10.2174/092986713804910175

M3 - Journal article

C2 - 23116145

AN - SCOPUS:84877814281

SN - 0929-8673

VL - 20

SP - 576

EP - 582

JO - Current Medicinal Chemistry

JF - Current Medicinal Chemistry

IS - 4

ER -

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

Abstract

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