Copper homeostasis is strictly regulated by protein transporters and chaperones, to allow its correct distribution and avoid uncontrolled redox reactions. Several studies address copper as involved in cancer development and spreading (epithelial to mesenchymal transition, angiogenesis). However, being endogenous and displaying a tremendous potential to generate free radicals, copper is a perfect candidate, once opportunely complexed, to be used as a drug in cancer therapy with low adverse effects. Copper ions can be modulated by the organic counterpart, after complexed to their metalcore, either in redox potential or geometry and consequently reactivity. During the last four decades, many copper complexes were studied regarding their reactivity toward cancer cells, and many of them could be a drug choice for phase II and III in cancer therapy. Also, there is promising evidence of using 64Cu in nanoparticles as radiopharmaceuticals for both positron emission tomography (PET) imaging and treatment of hypoxic tumors. However, few compounds have gone beyond testing in animal models, and none of them got the status of a drug for cancer chemotherapy. The main challenge is their solubility in physiological buffers and their different and non-predictable mechanism of action. Moreover, it is difficult to rationalize a structure-based activity for drug design and delivery. In this review, we describe the role

da Silva, D.a., De Luca, A., Squitti, R., Rongioletti, M., Rossi, L., Machado, C., et al. (2022). Copper in tumors and the use of copper-based compounds in cancer treatment. JOURNAL OF INORGANIC BIOCHEMISTRY, 226, 111634 [10.1016/j.jinorgbio.2021.111634].

Copper in tumors and the use of copper-based compounds in cancer treatment

De Luca A.
Membro del Collaboration Group
;
Rossi L.
Membro del Collaboration Group
;
2022-01-01

Abstract

Copper homeostasis is strictly regulated by protein transporters and chaperones, to allow its correct distribution and avoid uncontrolled redox reactions. Several studies address copper as involved in cancer development and spreading (epithelial to mesenchymal transition, angiogenesis). However, being endogenous and displaying a tremendous potential to generate free radicals, copper is a perfect candidate, once opportunely complexed, to be used as a drug in cancer therapy with low adverse effects. Copper ions can be modulated by the organic counterpart, after complexed to their metalcore, either in redox potential or geometry and consequently reactivity. During the last four decades, many copper complexes were studied regarding their reactivity toward cancer cells, and many of them could be a drug choice for phase II and III in cancer therapy. Also, there is promising evidence of using 64Cu in nanoparticles as radiopharmaceuticals for both positron emission tomography (PET) imaging and treatment of hypoxic tumors. However, few compounds have gone beyond testing in animal models, and none of them got the status of a drug for cancer chemotherapy. The main challenge is their solubility in physiological buffers and their different and non-predictable mechanism of action. Moreover, it is difficult to rationalize a structure-based activity for drug design and delivery. In this review, we describe the role
gen-2022
Pubblicato
Rilevanza internazionale
Articolo
Esperti anonimi
Settore BIO/12 - BIOCHIMICA CLINICA E BIOLOGIA MOLECOLARE CLINICA
English
Cancer
Copper in cancer
Cancer therapy
Copper complexes copper in medicine
Radiotherapy
Copper in tumor
https://www.sciencedirect.com/science/article/pii/S0162013421002816?via=ihub
da Silva, D.a., De Luca, A., Squitti, R., Rongioletti, M., Rossi, L., Machado, C., et al. (2022). Copper in tumors and the use of copper-based compounds in cancer treatment. JOURNAL OF INORGANIC BIOCHEMISTRY, 226, 111634 [10.1016/j.jinorgbio.2021.111634].
da Silva, Da; De Luca, A; Squitti, R; Rongioletti, M; Rossi, L; Machado, Cml; Cerchiaro, G
Articolo su rivista
File in questo prodotto:
File Dimensione Formato  
Da Silva et al. J Inorg Biochemistry 2022.pdf

solo utenti autorizzati

Tipologia: Versione Editoriale (PDF)
Licenza: Copyright dell'editore
Dimensione 5.35 MB
Formato Adobe PDF
5.35 MB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2108/288869
Citazioni
  • ???jsp.display-item.citation.pmc??? 53
  • Scopus 99
  • ???jsp.display-item.citation.isi??? 93
social impact