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Open AccessFeature PaperArticle

Selectivity of Terpyridine Platinum Anticancer Drugs for G-quadruplex DNA

Institut Curie, PSL Research University, CNRS-UMR 9187, INSERM U1196, F-91405 Orsay, France
Université Paris Sud, Université Paris-Saclay, CNRS-UMR 9187, INSERM U1196, F-91405 Orsay, France
University Rennes, CNRS, ISCR-UMR 6226, F-35000 Rennes, France
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Danzhou Yang
Molecules 2019, 24(3), 404;
Received: 14 December 2018 / Revised: 18 January 2019 / Accepted: 22 January 2019 / Published: 23 January 2019
(This article belongs to the Special Issue G-Quadruplex Ligands and Cancer)
Guanine-rich DNA can form four-stranded structures called G-quadruplexes (G4s) that can regulate many biological processes. Metal complexes have shown high affinity and selectivity toward the quadruplex structure. Here, we report the comparison of a panel of platinum (II) complexes for quadruplex DNA selective recognition by exploring the aromatic core around terpyridine derivatives. Their affinity and selectivity towards G4 structures of various topologies have been evaluated by FRET-melting (Fluorescence Resonance Energy Transfert-melting) and Fluorescent Intercalator Displacement (FID) assays, the latter performed by using three different fluorescent probes (Thiazole Orange (TO), TO-PRO-3, and PhenDV). Their ability to bind covalently to the c-myc G4 structure in vitro and their cytotoxicity potential in two ovarian cancerous cell lines were established. Our results show that the aromatic surface of the metallic ligands governs, in vitro, their affinity, their selectivity for the G4 over the duplex structures, and platination efficiency. However, the structural modifications do not allow significant discrimination among the different G4 topologies. Moreover, all compounds were tested on ovarian cancer cell lines and normal cell lines and were all able to overcome cisplatin resistance highlighting their interest as new anticancer drugs. View Full-Text
Keywords: terpyridine platinum complexes; G-quadruplex terpyridine platinum complexes; G-quadruplex
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MDPI and ACS Style

Morel, E.; Beauvineau, C.; Naud-Martin, D.; Landras-Guetta, C.; Verga, D.; Ghosh, D.; Achelle, S.; Mahuteau-Betzer, F.; Bombard, S.; Teulade-Fichou, M.-P. Selectivity of Terpyridine Platinum Anticancer Drugs for G-quadruplex DNA. Molecules 2019, 24, 404.

AMA Style

Morel E, Beauvineau C, Naud-Martin D, Landras-Guetta C, Verga D, Ghosh D, Achelle S, Mahuteau-Betzer F, Bombard S, Teulade-Fichou M-P. Selectivity of Terpyridine Platinum Anticancer Drugs for G-quadruplex DNA. Molecules. 2019; 24(3):404.

Chicago/Turabian Style

Morel, Elodie; Beauvineau, Claire; Naud-Martin, Delphine; Landras-Guetta, Corinne; Verga, Daniela; Ghosh, Deepanjan; Achelle, Sylvain; Mahuteau-Betzer, Florence; Bombard, Sophie; Teulade-Fichou, Marie-Paule. 2019. "Selectivity of Terpyridine Platinum Anticancer Drugs for G-quadruplex DNA" Molecules 24, no. 3: 404.

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