Iron and Copper Intracellular Chelation as an Anticancer Drug Strategy Inorganics 2018, 6(4), 126; https://doi.org/10.3390/inorganics6040126
Kavita Gaur 1,†, Alexandra M. Vázquez-Salgado 2,†OrcID, Geraldo Duran-Camacho 1,†, Irivette Dominguez-Martinez 1,†, Josué A. Benjamín-Rivera 1,†, Lauren Fernández-Vega 1,†, Lesly Carmona Sarabia 1,†, Angelys Cruz García 1, Felipe Pé
rez-Deliz 1, José A. Méndez Román 1, Melissa Vega-Cartagena 1, Sergio A. Loza-Rosas 1, Xaymara Rodriguez Acevedo 1 and Arthur D. Tinoco 1,* OrcID
Department of Chemistry, University of Puerto Rico, Río Piedras Campus, Río Piedras, PR 00931, USA
Department of Biology, University of Puerto Rico, Río Piedras Campus, Río Piedras, PR 00931, USA
Received: 28 September 2018 / Revised: 24 November 2018 / Accepted: 29 November 2018 / Published: 30 November 2018
(This article belongs to the Special Issue Unconventional Anticancer Metallodrugs and Strategies to Improve their Pharmacological Profile)

Abstract
A very promising direction in the development of anticancer drugs is inhibiting the molecular pathways that keep cancer cells alive and able to metastasize. Copper and iron are two essential metals that play significant roles in the rapid proliferation
of cancer cells and several chelators have been studied to suppress the bioavailability of these metals in the cells. This review discusses the major contributions that Cu and Fe play in the progression and spreading of cancer and evaluates select Cu and
Fe chelators that demonstrate great promise as anticancer drugs. Efforts to improve the cellular delivery, efficacy, and tumor responsiveness of these chelators are also presented including a transmetallation strategy for dual targeting of Cu and Fe. To
elucidate the effectiveness and specificity of Cu and Fe chelators for treating cancer, analytical tools are described for measuring Cu and Fe levels and for tracking the metals in cells, tissue, and the body. View Full-Text https://www.mdpi.com/2304-
6740/6/4/126
Keywords: copper and iron chelators in cancer; transmetalation; metastasis; angiogenesis; metallomics
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
Gaur, K.; Vázquez-Salgado, A.M.; Duran-Camacho, G.; Dominguez-Martinez, I.; Benjamín-Rivera, J.A.; Fernández-Vega, L.; Carmona Sarabia, L.; Cruz García, A.; Pérez-Deliz, F.; Méndez Román, J.A.; Vega-Cartagena, M.; Loza-Rosas, S.A.; Rodriguez
Acevedo, X.; Tinoco, A.D. Iron and Copper Intracellular Chelation as an Anticancer Drug Strategy. Inorganics 2018, 6, 126.

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