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Progress of HDAC inhibitor panobinostat in the treatment of cancer

机译:HDAC抑制剂Panobinostat在癌症治疗中的研究进展

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摘要

Histone deacetylases are a class of enzymes that play important roles in post translational modifications of histones by deacetylating the lysine residues as well as interacting with various non-histone proteins. This type of enzymes is closely related to oncogenesis and has been proved to be attractive targets for designing novel anti-cancer agents. Over the last 10 years, a large number of HDACs have entered pre-clinical and/or clinical trials. Among these drug candidates, the pan-HDAC inhibitor, panobinostat demonstrated high therapeutic potential as monotherapy and combined therapy in both preclinical models and clinical cancer patients. In this review, we have mainly focused on the recent progress of the clinical studies about panobinostat, and discussed its anti-cancer effects and molecular rationale for the treatment strategies.
机译:组蛋白脱乙酰基酶是一类酶,通过使赖氨酸残基脱乙酰基并与各种非组蛋白蛋白相互作用,在组蛋白的翻译后修饰中起重要作用。这种酶与肿瘤发生密切相关,并已被证明是设计新型抗癌药的有吸引力的靶标。在过去的十年中,大量的HDAC已进入临床前和/或临床试验。在这些候选药物中,pan-HDAC抑制剂panobinostat在临床前模型和临床癌症患者中均显示出作为单一疗法和联合疗法的高治疗潜力。在这篇综述中,我们主要关注有关panobinostat的临床研究的最新进展,并讨论其抗癌作用和治疗策略的分子原理。

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