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Epigenetics in Breast Cancer Therapy—New Strategies and Future Nanomedicine Perspectives

Cancer Research Institute, Biomedical Research Center of the Slovak Academy of Sciences, Dubravska Cesta 9, 845 05 Bratislava, Slovakia
Department of Clinical Dentistry, University of Bergen, Aarstadveien 19, 5009 Bergen, Norway
e-NIOS Applications Private Company, Alexandrou Pantou 25, 17671 Kallithea, Greece
Center of Systems Biology, Biomedical Research Foundation of the Academy of Athens, 11527 Athens, Greece
2nd Department of Oncology, Faculty of Medicine, Comenius University and National Cancer Institute, Klenova 1, 833 10 Bratislava, Slovakia
Latvian Institute of Organic Synthesis, Aizkraukles str. 21, LV-1006 Riga, Latvia
Health Effects Laboratory, NILU-Norwegian Institute for Air Research, 2007 Kjeller, Norway
Vall d Hebron, Institut de Recerca (VHIR), 08035 Barcelona, Spain
Institut Català de Nanosciència i Nanotecnologia (ICN2), Bellaterra, 08193 Barcelona, Spain
Institució Catalana de Recerca i Estudis Avançats (ICREA), 08010 Barcelona, Spain
Author to whom correspondence should be addressed.
Alena Gabelova and Bozena Smolkova share the senior authorship.
Cancers 2020, 12(12), 3622;
Received: 31 October 2020 / Revised: 30 November 2020 / Accepted: 30 November 2020 / Published: 3 December 2020
(This article belongs to the Special Issue Epigenetic Therapy: The State of Play in Highly Aggressive Diseases)
Despite advances in cancer treatment, difficult-to-treat tumor subtypes remain a challenge. New multidisciplinary approaches can help overcome current obstacles posed by tumor heterogeneity, activation and enrichment of cancer stem cells, and acquired drug resistance development. Epigenome modulation, currently unsuccessful in solid tumors due to epigenetic drug instability, toxicity, and off-target effects, might be enabled by implementing nano-based delivery strategies aiming to improve breast cancer patient outcomes.
Epigenetic dysregulation has been recognized as a critical factor contributing to the development of resistance against standard chemotherapy and to breast cancer progression via epithelial-to-mesenchymal transition. Although the efficacy of the first-generation epigenetic drugs (epi-drugs) in solid tumor management has been disappointing, there is an increasing body of evidence showing that epigenome modulation, in synergy with other therapeutic approaches, could play an important role in cancer treatment, reversing acquired therapy resistance. However, the epigenetic therapy of solid malignancies is not straightforward. The emergence of nanotechnologies applied to medicine has brought new opportunities to advance the targeted delivery of epi-drugs while improving their stability and solubility, and minimizing off-target effects. Furthermore, the omics technologies, as powerful molecular epidemiology screening tools, enable new diagnostic and prognostic epigenetic biomarker identification, allowing for patient stratification and tailored management. In combination with new-generation epi-drugs, nanomedicine can help to overcome low therapeutic efficacy in treatment-resistant tumors. This review provides an overview of ongoing clinical trials focusing on combination therapies employing epi-drugs for breast cancer treatment and summarizes the latest nano-based targeted delivery approaches for epi-drugs. Moreover, it highlights the current limitations and obstacles associated with applying these experimental strategies in the clinics. View Full-Text
Keywords: epigenetics; breast cancer; nanomedicine; epi-drugs; targeted delivery; drug resistance epigenetics; breast cancer; nanomedicine; epi-drugs; targeted delivery; drug resistance
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MDPI and ACS Style

Buocikova, V.; Rios-Mondragon, I.; Pilalis, E.; Chatziioannou, A.; Miklikova, S.; Mego, M.; Pajuste, K.; Rucins, M.; Yamani, N.E.; Longhin, E.M.; Sobolev, A.; Freixanet, M.; Puntes, V.; Plotniece, A.; Dusinska, M.; Cimpan, M.R.; Gabelova, A.; Smolkova, B. Epigenetics in Breast Cancer Therapy—New Strategies and Future Nanomedicine Perspectives. Cancers 2020, 12, 3622.

AMA Style

Buocikova V, Rios-Mondragon I, Pilalis E, Chatziioannou A, Miklikova S, Mego M, Pajuste K, Rucins M, Yamani NE, Longhin EM, Sobolev A, Freixanet M, Puntes V, Plotniece A, Dusinska M, Cimpan MR, Gabelova A, Smolkova B. Epigenetics in Breast Cancer Therapy—New Strategies and Future Nanomedicine Perspectives. Cancers. 2020; 12(12):3622.

Chicago/Turabian Style

Buocikova, Verona, Ivan Rios-Mondragon, Eleftherios Pilalis, Aristotelis Chatziioannou, Svetlana Miklikova, Michal Mego, Karlis Pajuste, Martins Rucins, Naouale E. Yamani, Eleonora M. Longhin, Arkadij Sobolev, Muriel Freixanet, Victor Puntes, Aiva Plotniece, Maria Dusinska, Mihaela R. Cimpan, Alena Gabelova, and Bozena Smolkova. 2020. "Epigenetics in Breast Cancer Therapy—New Strategies and Future Nanomedicine Perspectives" Cancers 12, no. 12: 3622.

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