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Communication

Protein-Based Delivery Systems for Anticancer Metallodrugs: Structure and Biological Activity of the Oxaliplatin/β-Lactoglobulin Adduct

1
Department of Chemical Sciences, University of Naples Federico II, Complesso Universitario di Monte Sant’Angelo, Via Cintia, 21, 80126 Napoli, Italy
2
CEINGE Advanced Biotechnologies s.c.a.r.l., Via G. Salvatore 486, 80145 Napoli, Italy
3
Department of Chemistry and Industrial Chemistry, University of Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2022, 15(4), 425; https://doi.org/10.3390/ph15040425
Submission received: 18 February 2022 / Revised: 21 March 2022 / Accepted: 28 March 2022 / Published: 30 March 2022

Abstract

β-lactoglobulin is the major component of whey. Here, the adduct formed upon the reaction of the protein with oxaliplatin (OXA) has been prepared, structurally characterized by X-ray crystallography and electrospray ionization–mass spectrometry, and evaluated as a cytotoxic agent. The data demonstrate that OXA rapidly binds β-lactoglobulin via coordination with a Met7 side chain upon release of the oxalate ligand. The adduct is significantly more cytotoxic than the free drug and induces apoptosis in cancer cells. Overall, our results suggest that metallodrug/β-lactoglobulin adducts can be used as anticancer agents and that the protein can be used as a metallodrug delivery system.
Keywords: delivery system; protein; metallodrug; anticancer; protein metalation delivery system; protein; metallodrug; anticancer; protein metalation
Graphical Abstract

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MDPI and ACS Style

Monti, D.M.; Loreto, D.; Iacobucci, I.; Ferraro, G.; Pratesi, A.; D’Elia, L.; Monti, M.; Merlino, A. Protein-Based Delivery Systems for Anticancer Metallodrugs: Structure and Biological Activity of the Oxaliplatin/β-Lactoglobulin Adduct. Pharmaceuticals 2022, 15, 425. https://doi.org/10.3390/ph15040425

AMA Style

Monti DM, Loreto D, Iacobucci I, Ferraro G, Pratesi A, D’Elia L, Monti M, Merlino A. Protein-Based Delivery Systems for Anticancer Metallodrugs: Structure and Biological Activity of the Oxaliplatin/β-Lactoglobulin Adduct. Pharmaceuticals. 2022; 15(4):425. https://doi.org/10.3390/ph15040425

Chicago/Turabian Style

Monti, Daria Maria, Domenico Loreto, Ilaria Iacobucci, Giarita Ferraro, Alessandro Pratesi, Luigi D’Elia, Maria Monti, and Antonello Merlino. 2022. "Protein-Based Delivery Systems for Anticancer Metallodrugs: Structure and Biological Activity of the Oxaliplatin/β-Lactoglobulin Adduct" Pharmaceuticals 15, no. 4: 425. https://doi.org/10.3390/ph15040425

APA Style

Monti, D. M., Loreto, D., Iacobucci, I., Ferraro, G., Pratesi, A., D’Elia, L., Monti, M., & Merlino, A. (2022). Protein-Based Delivery Systems for Anticancer Metallodrugs: Structure and Biological Activity of the Oxaliplatin/β-Lactoglobulin Adduct. Pharmaceuticals, 15(4), 425. https://doi.org/10.3390/ph15040425

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