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CD133-Functionalized Gold Nanoparticles as a Carrier Platform for Telaglenastat (CB-839) against Tumor Stem Cells

Department of Neurology, Faculty of Medicine, Heinrich-Heine-University, 40225 Düsseldorf, Germany
Institut für Anorganische Chemie und Strukturchemie, Heinrich-Heine-University, 40204 Düsseldorf, Germany
Molecular and Experimental Surgery, University Clinic for General-, Visceral-, Vascular- and Transplantation Surgery, Faculty of Medicine, Otto-von-Guericke-University, 39120 Magdeburg, Germany
Clinic for Neurosurgery, Heinrich-Heine-University, 40225 Düsseldorf, Germany
Department of Radiopharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 1416634793, Iran
Institute of Chemical Biology and Fundamental Medicine SB RAS, 630090 Novosibirsk, Russia
Laboratoire de Chimie de Coordination CNRS, 31400 Toulouse, France
Epilepsy Research Center, Department of Neurosurgery and Department of Neurology, Westfälische Wilhelms-Universität, 48149 Münster, Germany
Shefa Neuroscience Research Center, Khatam Alanbia Hospital, Tehran 9815733169, Iran
Authors to whom correspondence should be addressed.
Academic Editors: Rolf Heumann and Frank Schmitz
Int. J. Mol. Sci. 2022, 23(10), 5479;
Received: 7 April 2022 / Revised: 4 May 2022 / Accepted: 9 May 2022 / Published: 13 May 2022
(This article belongs to the Collection State-of-the-Art Molecular Neurobiology in Germany)
The failure of a long-lasting curative therapeutic benefit of currently applied chemotherapies against malignant cancers is suggested to be caused by the ineffectiveness of such interventions on cancer stem cells (CSCs). CD133/AC133 is a cell surface protein previously shown to have potential to identify CSCs in various tumors, including brain tumors. Moreover, an increase in the rate of cellular metabolism of glutamine and glucose are contributors to the fast cellular proliferation of some high-grade malignancies. Inhibition of glutaminolysis by utilizing pharmacological inhibitors of the enzyme glutaminase 1 (GLS1) can be an effective anti-CSC strategy. In this study, the clinical-stage GLS1 inhibitor Telaglenastat (CB-839) was loaded into PEGylated gold nanoparticles equipped with the covalently conjugated CD133 aptamer (Au-PEG-CD133-CB-839) and exposed to a collection of CD133-positive brain tumor models in vitro. Our results show that Au-PEG-CD133-CB-839 significantly decreased the viability of CD133-postive cancer cells in a dose-dependent manner, which was higher as compared to the effects of treatment of the cells with the individual components of the assembled nanodrug. Interestingly, the treatment effect was observed in glioblastoma stem cells modeling different transcriptomic subtypes of the disease. The presented platform is the fundament for subsequent target specificity characterization and in vivo application. View Full-Text
Keywords: cancer stem cells; nanomedicine; glutaminase; onco-metabolism; CD133 cancer stem cells; nanomedicine; glutaminase; onco-metabolism; CD133
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MDPI and ACS Style

Poonaki, E.; Nickel, A.-C.; Shafiee Ardestani, M.; Rademacher, L.; Kaul, M.; Apartsin, E.; Meuth, S.G.; Gorji, A.; Janiak, C.; Kahlert, U.D. CD133-Functionalized Gold Nanoparticles as a Carrier Platform for Telaglenastat (CB-839) against Tumor Stem Cells. Int. J. Mol. Sci. 2022, 23, 5479.

AMA Style

Poonaki E, Nickel A-C, Shafiee Ardestani M, Rademacher L, Kaul M, Apartsin E, Meuth SG, Gorji A, Janiak C, Kahlert UD. CD133-Functionalized Gold Nanoparticles as a Carrier Platform for Telaglenastat (CB-839) against Tumor Stem Cells. International Journal of Molecular Sciences. 2022; 23(10):5479.

Chicago/Turabian Style

Poonaki, Elham, Ann-Christin Nickel, Mehdi Shafiee Ardestani, Lars Rademacher, Marilyn Kaul, Evgeny Apartsin, Sven G. Meuth, Ali Gorji, Christoph Janiak, and Ulf D. Kahlert. 2022. "CD133-Functionalized Gold Nanoparticles as a Carrier Platform for Telaglenastat (CB-839) against Tumor Stem Cells" International Journal of Molecular Sciences 23, no. 10: 5479.

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