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Article

Antitumor Activity of Nanoparticles Loaded with PHT-427, a Novel AKT/PDK1 Inhibitor, for the Treatment of Head and Neck Squamous Cell Carcinoma

1
Department Otolaryngology, Hospital Universitario de Getafe, Getafe (Madrid), Carretera de Toledo, km 12.500, 28905 Madrid, Spain
2
Department of Polymeric Nanomaterials and Biomaterials Institute of Polymer Science and Technology CSIC, C/Juan de la Cierva, 3, 28006 Madrid, Spain
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Biomedical Research Centre in Bioengineering Biomaterials, and Nanomedicine CIBER-BBN, 28029 Madrid, Spain
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Department of Medicine, Faculty of Biomedical and Health Sciences, Universidad Europea de Madrid, Villaviciosa de Odón, 28670 Madrid, Spain
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Fundación de Investigación Biomédica del Hospital Universitario de Getafe, Carretera de Toledo, km 12.500, 28905 Madrid, Spain
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CIBER de Enfermedades Respiratorias, Instituto de Investigación Carlos III, 28029 Madrid, Spain
*
Author to whom correspondence should be addressed.
Academic Editors: Sílvia Castro Coelho and Manuel A.N. Coelho
Pharmaceutics 2021, 13(8), 1242; https://doi.org/10.3390/pharmaceutics13081242
Received: 5 July 2021 / Revised: 3 August 2021 / Accepted: 7 August 2021 / Published: 12 August 2021
(This article belongs to the Special Issue Nanocarriers for Cancer Therapy and Diagnosis)
Currently, new treatments are required to supplement the current standard of care for head and neck squamous cell carcinoma (HNSCC). The phosphatidylinositol3-kinase (PI3K) signaling pathway is commonly altered and activated in HNSCC. PHT-427 is a dual PI3K-mammalian target of the AKT/PDK1 inhibitor; however, to the best of our knowledge, the effect of the PHT-427 inhibitor on HNSCC has not been investigated. This study aims to evaluate the antitumoral effect of PHT-427-loaded polymeric nanoparticles based on α-tocopheryl succinate (α-TOS). The in vitro activity of PHT-427 was tested in hypopharynx carcinoma squamous cells (FaDu) to measure the cell viability, PI3KCA/AKT/PDK1 gene expression, and PI3KCA/AKT/PDK1 levels. Apoptosis, epidermal growth factor receptor (EGFR), and reactive oxygen species (ROS) were also measured. The presence of PHT-427 significantly enhances its antiproliferative and proapoptotic activity by inactivating the PI3K/AKT/PDK1 pathway. Nanoparticles (NPs) effectively suppress AKT/PDK1 expression. Additionally, NPs loaded with PHT-427 produce high oxidative stress levels that induce apoptosis. In conclusion, these results are promising in the use of this nanoformulation as a PHT-427 delivery system for effective HNSCC treatment. View Full-Text
Keywords: PHT-427 inhibitor; polymeric nanoparticle; PI3K pathway; AKT; PDK1; hypopharynx carcinoma squamous cells PHT-427 inhibitor; polymeric nanoparticle; PI3K pathway; AKT; PDK1; hypopharynx carcinoma squamous cells
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MDPI and ACS Style

Yanes-Díaz, J.; Palao-Suay, R.; Aguilar, M.R.; Riestra-Ayora, J.I.; Ferruelo-Alonso, A.; Rojo del Olmo, L.; Vázquez-Lasa, B.; Sanz-Fernández, R.; Sánchez-Rodríguez, C. Antitumor Activity of Nanoparticles Loaded with PHT-427, a Novel AKT/PDK1 Inhibitor, for the Treatment of Head and Neck Squamous Cell Carcinoma. Pharmaceutics 2021, 13, 1242. https://doi.org/10.3390/pharmaceutics13081242

AMA Style

Yanes-Díaz J, Palao-Suay R, Aguilar MR, Riestra-Ayora JI, Ferruelo-Alonso A, Rojo del Olmo L, Vázquez-Lasa B, Sanz-Fernández R, Sánchez-Rodríguez C. Antitumor Activity of Nanoparticles Loaded with PHT-427, a Novel AKT/PDK1 Inhibitor, for the Treatment of Head and Neck Squamous Cell Carcinoma. Pharmaceutics. 2021; 13(8):1242. https://doi.org/10.3390/pharmaceutics13081242

Chicago/Turabian Style

Yanes-Díaz, Joaquín, Raquel Palao-Suay, María R. Aguilar, Juan I. Riestra-Ayora, Antonio Ferruelo-Alonso, Luis Rojo del Olmo, Blanca Vázquez-Lasa, Ricardo Sanz-Fernández, and Carolina Sánchez-Rodríguez. 2021. "Antitumor Activity of Nanoparticles Loaded with PHT-427, a Novel AKT/PDK1 Inhibitor, for the Treatment of Head and Neck Squamous Cell Carcinoma" Pharmaceutics 13, no. 8: 1242. https://doi.org/10.3390/pharmaceutics13081242

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