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Cited by 206

The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.

A Platinum Supramolecular Square as an Effective G-Quadruplex Binder and Telomerase Inhibitor

Kieltyka, Roxanne, Englebienne, Pablo, Fakhoury, Johans, Autexier, Chantal, Moitessier, Nicolas, Sleiman, Hanadi F.·2008·Journal of the American Chemical Society

Abstract

In this contribution, we report that a self-assembled platinum molecular square [Pt(en)(4,4'-dipyridyl)]4 can act as an efficient G-quadruplex binder and telomerase inhibitor. Molecular modeling studies show that the square arrangement of the four bipyridyl ligands, the highly electropositive nature of the overall complex, as well as hydrogen bonding interactions between the ethylenediamine ligands and phosphates of the DNA backbone all contribute to the observed strong binding affinity to the G-quadruplex. Through thermal denaturation studies with duplex and quadruplex FRET probes and enzymatic assays, we demonstrate that this platinum square strongly binds to G-quadruplexes and can act as an inhibitor of telomerase. This study thus shows the potential of supramolecular self-assembly to readily generate scaffolds of unique geometries for effective targeting of G-quadruplexes and for the ultimate development of selective antitumor therapies.

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Metadata

Authors
Kieltyka, R., Englebienne, P., Fakhoury, J., Autexier, C., Moitessier, N., & Sleiman, H. F.
Venue
Journal of the American Chemical Society
Published
2008-07-11
Volume
130
Issue
31
Pages
10040-10041
ISSN
  • 0002-7863 (ISSN-L)
  • 1520-5126
OpenAlex
W2054402484
Cited by
206
References
1
FWCI
6.82
Type
journal article
Language
en
Open access
closed

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