Beljkas Milan, Ilic Aleksandra, Cebzan Alen, Radovic Branko, Djokovic Nemanja, Ruzic Dusan, Nikolic Katarina, Oljacic Slavica
Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
Pharmaceutics. 2023 Nov 3;15(11):2581. doi: 10.3390/pharmaceutics15112581.
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.
组蛋白去乙酰化酶（HDACs）是组蛋白和非组蛋白蛋白质乙酰化平衡的主要调节因子。与其他HDAC亚型不同，HDAC6主要参与维持许多非组蛋白蛋白质的乙酰化平衡。因此，HDAC6的过表达与各种恶性肿瘤的发生、侵袭、迁移、存活、凋亡和生长有关。因此，HDAC6被认为是癌症治疗的一个有前景的靶点。然而，目前尚无选择性HDAC6抑制剂用于临床，主要原因是其显示抗癌特性所需的浓度高且疗效低，这可能导致脱靶效应。因此，具有双靶点能力的HDAC6抑制剂代表了癌症治疗的新趋势，旨在克服上述问题。在这篇综述中，我们总结了双靶点HDAC6抑制剂在肿瘤治疗方面的进展。
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