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Biomimetic Magnetic Nanocarriers Drive Choline Kinase Alpha Inhibitor inside Cancer Cells for Combined Chemo-Hyperthermia Therapy

1
Department of Microbiology, Faculty of Sciences, University of Granada, 18071 Granada, Spain
2
Department of Biochemistry and Molecular Biology I, Faculty of Sciences, University of Granada, 18071 Granada, Spain
3
Department of Neurosciences, Biomedicine and Movement Sciences, Anatomy and Histology Section, University of Verona, 37134 Verona, Italy
4
Department of Applied Physics, Faculty of Sciences, University of Granada, 18071 Granada, Spain
5
Department of Pharmaceutical and Organic Chemistry, Faculty of Pharmacy, Campus of Cartuja, 18071 Granada, Spain
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceutics 2019, 11(8), 408; https://doi.org/10.3390/pharmaceutics11080408
Received: 2 July 2019 / Revised: 1 August 2019 / Accepted: 8 August 2019 / Published: 12 August 2019
(This article belongs to the Special Issue Nanopharmaceuticals for Image-Guided Cancer Therapy and Diagnosis)
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Abstract

Choline kinase α1 (ChoKα1) has become an excellent antitumor target. Among all the inhibitors synthetized, the new compound Ff35 shows an excellent capacity to inhibit ChoKα1 activity. However, soluble Ff35 is also capable of inhibiting choline uptake, making the inhibitor not selective for ChoKα1. In this study, we designed a new protocol with the aim of disentangling whether the Ff35 biological action is due to the inhibition of the enzyme and/or to the choline uptake. Moreover, we offer an alternative to avoid the inhibition of choline uptake caused by Ff35, since the coupling of Ff35 to novel biomimetic magnetic nanoparticles (BMNPs) allows it to enter the cell through endocytosis without interacting with the choline transporter. This opens the possibility of a clinical use of Ff35. Our results indicate that Ff35-BMNPs nanoassemblies increase the selectivity of Ff35 and have an antiproliferative effect. Also, we demonstrate the effectiveness of the tandem Ff35-BMNPs and hyperthermia. View Full-Text
Keywords: biomimetic; magnetic nanoparticle; ChoKα1 inhibitor; Ff35; drug delivery; hyperthermia biomimetic; magnetic nanoparticle; ChoKα1 inhibitor; Ff35; drug delivery; hyperthermia
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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).
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Jabalera, Y.; Sola-Leyva, A.; Peigneux, A.; Vurro, F.; Iglesias, G.R.; Vilchez-Garcia, J.; Pérez-Prieto, I.; Aguilar-Troyano, F.J.; López-Cara, L.C.; Carrasco-Jiménez, M.P.; Jimenez-Lopez, C. Biomimetic Magnetic Nanocarriers Drive Choline Kinase Alpha Inhibitor inside Cancer Cells for Combined Chemo-Hyperthermia Therapy. Pharmaceutics 2019, 11, 408.

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