Exclusive platination of loop adenines in the human telomeric G-quadruplex

The present article reports on the platination of the human telomeric G-quadruplex by three Pt-terpyridine complexes. It is shown that extension of the aromatic surface of the terpyridine moiety surrounding the platinum atom influences both the binding affinity and the platination activity. Remarkab...

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Published inOrganic & biomolecular chemistry Vol. 7; no. 14; pp. 2864 - 2871
Main Authors Bertrand, Hélène, Bombard, Sophie, Monchaud, David, Talbot, Eric, Guédin, Aurore, Mergny, Jean-Louis, Grünert, Renate, Bednarski, Patrick J, Teulade-Fichou, Marie-Paule
Format Journal Article
LanguageEnglish
Published England Royal Society of Chemistry 01.01.2009
Subjects
Adenine - chemistry
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Base Sequence
Biochemistry, Molecular Biology
Cell Line, Tumor
Cell Proliferation - drug effects
Circular Dichroism
G-Quadruplexes
Humans
Life Sciences
Models, Molecular
Nucleic Acid Conformation
Organometallic Compounds - chemistry
Organometallic Compounds - pharmacology
Platinum - chemistry
Platinum - pharmacology
Substrate Specificity
Telomere - chemistry
Telomere - genetics
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Summary:The present article reports on the platination of the human telomeric G-quadruplex by three Pt-terpyridine complexes. It is shown that extension of the aromatic surface of the terpyridine moiety surrounding the platinum atom influences both the binding affinity and the platination activity. Remarkably, the most strongly bound complex Pt-ttpy coordinates exclusively the adenine nucleobases present in the loop of the G-quadruplex. This exclusive single-site platination reflects the interaction of the compound with both the G-tetrad and the loop residues. In addition Pt-ttpy showed promising antiproliferative activity on a panel of cancer cell lines in a parallel study using cisplatin derivatives currently in clinical use.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:1477-0520
1477-0539
DOI:10.1039/b904599f