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Open AccessArticle

In Cellulo Evaluation of the Therapeutic Potential of NHC Platinum Compounds in Metastatic Cutaneous Melanoma

1
Hospices Civils de Lyon, EA3738-Therapeutic Targeting in Oncology, Université Jean Monnet-Université Claude Bernard Lyon1, 165 Chemin du Grand Revoyet, CEDEX, 69921 Oullins, France
2
INSERM 1052, CNRS 5286, Centre Léon Bérard, Centre de Recherche en Cancérologie de Lyon, Université de Lyon, Université Claude Bernard Lyon1, CEDEX 08, 69373 Lyon, France
3
Institut de Physique et Chimie des Matériaux de Strasbourg, Université de Strasbourg-CNRS UMR7504, Strasbourg, Bâtiment 69, 23 Rue du Loess, 67200 Strasbourg, France
4
Hôpital Nord, Département de Pharmacie, Centre Hospitalier Universitaire de Saint-Etienne, Avenue Albert Raimond, 42270 Saint-Priest, France
5
Cancer Cell Death Laboratory, part of LabEx DEVweCAN, Cancer Initiation and Tumoral Cell Identity Department, Centre de Recherche en Cancérologie de Lyon, 69008 Lyon, France
6
Laboratoire de Géologie de Lyon Terre, Planètes, Université de Lyon, Environnement-ENS-UCBL-CNRS, UMR CNRS 5276 (CNRS, ENS, Université Lyon1), École Normale Supérieure de Lyon, 9 rue du Vercors, CEDEX 07, 69364 Lyon, France
7
École Normale Supérieure de Lyon, Université de Lyon, 9 rue du Vercors, CEDEX 07, 69364 Lyon, France
8
UFR de Médecine, Campus Santé Innovations, Université de Lyon, Université Jean Monnet, 10 rue de Marandière, 42270 Saint-Priest en Jarez, France
*
Author to whom correspondence should be addressed.
Co-senior authors.
Int. J. Mol. Sci. 2020, 21(21), 7826; https://doi.org/10.3390/ijms21217826
Received: 7 September 2020 / Revised: 8 October 2020 / Accepted: 19 October 2020 / Published: 22 October 2020
(This article belongs to the Special Issue Skin Cancer and Melanoma)
We describe here the evaluation of the cytotoxic efficacy of two platinum (II) complexes bearing an N-heterocyclic carbene (NHC) ligand, a pyridine ligand and bromide or iodide ligands on a panel of human metastatic cutaneous melanoma cell lines representing different genetic subsets including BRAF-inhibitor-resistant cell lines, namely A375, SK-MEL-28, MeWo, HMCB, A375-R, SK-MEL-5-R and 501MEL-R. Cisplatin and dacarbazine were also studied for comparison purposes. Remarkably, the iodine-labelled Pt-NHC complex strongly inhibited proliferation of all tested melanoma cells after 1-h exposure, likely due to its rapid uptake by melanoma cells. The mechanism of this inhibitory activity involves the formation of DNA double-strand breaks and apoptosis. Considering the intrinsic chemoresistance of metastatic melanoma cells of current systemic treatments, these findings are promising and could give research opportunities in the future to improve the prognosis of patients suffering from unresectable metastatic melanoma that are not eligible or that do not respond to the most effective drugs available to date, namely BRAF inhibitors and the anti-PD-1 monoclonal antibody (mAb). View Full-Text
Keywords: platinum N-heterocyclic carbene complexes; metastatic cutaneous melanoma; chemotherapy; BRAF inhibitor resistance; apoptosis; chemoresistance platinum N-heterocyclic carbene complexes; metastatic cutaneous melanoma; chemotherapy; BRAF inhibitor resistance; apoptosis; chemoresistance
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MDPI and ACS Style

Charignon, E.; Bouché, M.; Clave-Darcissac, C.; Dahm, G.; Ichim, G.; Clotagatide, A.; Mertani, H.C.; Telouk, P.; Caramel, J.; Diaz, J.-J.; Bellemin-Laponnaz, S.; Bouvet, P.; Billotey, C. In Cellulo Evaluation of the Therapeutic Potential of NHC Platinum Compounds in Metastatic Cutaneous Melanoma. Int. J. Mol. Sci. 2020, 21, 7826. https://doi.org/10.3390/ijms21217826

AMA Style

Charignon E, Bouché M, Clave-Darcissac C, Dahm G, Ichim G, Clotagatide A, Mertani HC, Telouk P, Caramel J, Diaz J-J, Bellemin-Laponnaz S, Bouvet P, Billotey C. In Cellulo Evaluation of the Therapeutic Potential of NHC Platinum Compounds in Metastatic Cutaneous Melanoma. International Journal of Molecular Sciences. 2020; 21(21):7826. https://doi.org/10.3390/ijms21217826

Chicago/Turabian Style

Charignon, Elsa; Bouché, Mathilde; Clave-Darcissac, Caroline; Dahm, Georges; Ichim, Gabriel; Clotagatide, Anthony; Mertani, Hichem C.; Telouk, Philippe; Caramel, Julie; Diaz, Jean-Jacques; Bellemin-Laponnaz, Stéphane; Bouvet, Philippe; Billotey, Claire. 2020. "In Cellulo Evaluation of the Therapeutic Potential of NHC Platinum Compounds in Metastatic Cutaneous Melanoma" Int. J. Mol. Sci. 21, no. 21: 7826. https://doi.org/10.3390/ijms21217826

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