In Cellulo Evaluation of the Therapeutic Potential of NHC Platinum Compounds in Metastatic Cutaneous Melanoma - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue International Journal of Molecular Sciences Année : 2020

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

Elsa Charignon
  • Fonction : Auteur
Mathilde Bouché
Caroline Clave-Darcissac
  • Fonction : Auteur
Georges Dahm
  • Fonction : Auteur
Gabriel Ichim
Anthony Clotagatide
Hichem Mertani
Philippe Telouk
  • Fonction : Auteur
Julie Caramel
Jean-Jacques Diaz
Stéphane Bellemin-Laponnaz
Philippe Bouvet
Claire Billotey
  • Fonction : Auteur

Résumé

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).
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Dates et versions

hal-03011335 , version 1 (25-11-2020)

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Elsa Charignon, Mathilde Bouché, Caroline Clave-Darcissac, Georges Dahm, Gabriel Ichim, et al.. In Cellulo Evaluation of the Therapeutic Potential of NHC Platinum Compounds in Metastatic Cutaneous Melanoma. International Journal of Molecular Sciences, 2020, 21 (21), pp.7826. ⟨10.3390/ijms21217826⟩. ⟨hal-03011335⟩
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