Targeting Histone Deacetylases 6 in Dual-Target Therapy of Cancer
Authors
Beljkaš, MilanIlić, Aleksandra
Cebzan, Alen
Radović, Branko
Đoković, Nemanja
Ružić, Dušan
Nikolić, Katarina
Oljačić, Slavica
Article (Published version)
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Show full item recordAbstract
Histone deacetylases (HDACs) are the major regulators of the balance of acetylation of histone and non-histone proteins. In contrast to other HDAC isoforms, HDAC6 is mainly involved in maintaining the acetylation balance of many non-histone proteins. Therefore, the overexpression of HDAC6 is associated with tumorigenesis, invasion, migration, survival, apoptosis and growth of various malignancies. As a result, HDAC6 is considered a promising target for cancer treatment. However, none of selective HDAC6 inhibitors are in clinical use, mainly because of the low efficacy and high concentrations used to show anticancer properties, which may lead to off-target effects. Therefore, HDAC6 inhibitors with dual-target capabilities represent a new trend in cancer treatment, aiming to overcome the above problems. In this review, we summarize the advances in tumor treatment with dual-target HDAC6 inhibitors.
Keywords:
cancer / epigenetics / histone deacetylases / dual-target therapy / inhibitors / kinases / rational designSource:
Pharmaceutics, 2023, 15, 11Publisher:
- MDPI
Funding / projects:
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200161 (University of Belgrade, Faculty of Pharmacy) (RS-MESTD-inst-2020-200161)
DOI: 10.3390/pharmaceutics15112581
ISSN: 1999-4923
PubMed: 38004560
Scopus: 2-s2.0-85178378286
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Institution/Community
PharmacyTY - JOUR AU - Beljkaš, Milan AU - Ilić, Aleksandra AU - Cebzan, Alen AU - Radović, Branko AU - Đoković, Nemanja AU - Ružić, Dušan AU - Nikolić, Katarina AU - Oljačić, Slavica PY - 2023 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/5339 AB - Histone deacetylases (HDACs) are the major regulators of the balance of acetylation of histone and non-histone proteins. In contrast to other HDAC isoforms, HDAC6 is mainly involved in maintaining the acetylation balance of many non-histone proteins. Therefore, the overexpression of HDAC6 is associated with tumorigenesis, invasion, migration, survival, apoptosis and growth of various malignancies. As a result, HDAC6 is considered a promising target for cancer treatment. However, none of selective HDAC6 inhibitors are in clinical use, mainly because of the low efficacy and high concentrations used to show anticancer properties, which may lead to off-target effects. Therefore, HDAC6 inhibitors with dual-target capabilities represent a new trend in cancer treatment, aiming to overcome the above problems. In this review, we summarize the advances in tumor treatment with dual-target HDAC6 inhibitors. PB - MDPI T2 - Pharmaceutics T1 - Targeting Histone Deacetylases 6 in Dual-Target Therapy of Cancer VL - 15 IS - 11 DO - 10.3390/pharmaceutics15112581 ER -
@article{ author = "Beljkaš, Milan and Ilić, Aleksandra and Cebzan, Alen and Radović, Branko and Đoković, Nemanja and Ružić, Dušan and Nikolić, Katarina and Oljačić, Slavica", year = "2023", abstract = "Histone deacetylases (HDACs) are the major regulators of the balance of acetylation of histone and non-histone proteins. In contrast to other HDAC isoforms, HDAC6 is mainly involved in maintaining the acetylation balance of many non-histone proteins. Therefore, the overexpression of HDAC6 is associated with tumorigenesis, invasion, migration, survival, apoptosis and growth of various malignancies. As a result, HDAC6 is considered a promising target for cancer treatment. However, none of selective HDAC6 inhibitors are in clinical use, mainly because of the low efficacy and high concentrations used to show anticancer properties, which may lead to off-target effects. Therefore, HDAC6 inhibitors with dual-target capabilities represent a new trend in cancer treatment, aiming to overcome the above problems. In this review, we summarize the advances in tumor treatment with dual-target HDAC6 inhibitors.", publisher = "MDPI", journal = "Pharmaceutics", title = "Targeting Histone Deacetylases 6 in Dual-Target Therapy of Cancer", volume = "15", number = "11", doi = "10.3390/pharmaceutics15112581" }
Beljkaš, M., Ilić, A., Cebzan, A., Radović, B., Đoković, N., Ružić, D., Nikolić, K.,& Oljačić, S.. (2023). Targeting Histone Deacetylases 6 in Dual-Target Therapy of Cancer. in Pharmaceutics MDPI., 15(11). https://doi.org/10.3390/pharmaceutics15112581
Beljkaš M, Ilić A, Cebzan A, Radović B, Đoković N, Ružić D, Nikolić K, Oljačić S. Targeting Histone Deacetylases 6 in Dual-Target Therapy of Cancer. in Pharmaceutics. 2023;15(11). doi:10.3390/pharmaceutics15112581 .
Beljkaš, Milan, Ilić, Aleksandra, Cebzan, Alen, Radović, Branko, Đoković, Nemanja, Ružić, Dušan, Nikolić, Katarina, Oljačić, Slavica, "Targeting Histone Deacetylases 6 in Dual-Target Therapy of Cancer" in Pharmaceutics, 15, no. 11 (2023), https://doi.org/10.3390/pharmaceutics15112581 . .