Department of Medicine, Division of Infectious Diseases, University of Colorado Denver, Aurora, Colorado 80045, USA.
Mol Med. 2011 May-Jun;17(5-6):333-52. doi: 10.2119/molmed.2011.00116. Epub 2011 May 5.
This issue of Molecular Medicine contains 14 original research reports and state-of-the-art reviews on histone deacetylase inhibitors (HDACi's), which are being studied in models of a broad range of diseases not related to the proapoptotic properties used to treat cancer. The spectrum of these diseases responsive to HDACi's is for the most part due to several antiinflammatory properties, often observed in vitro but importantly also in animal models. One unifying property is a reduction in cytokine production as well as inhibition of cytokine postreceptor signaling. Distinct from their use in cancer, the reduction in inflammation by HDACi's is consistently observed at low concentrations compared with the higher concentrations required for killing tumor cells. This characteristic makes HDACi's attractive candidates for treating chronic diseases, since low doses are well tolerated. For example, low oral doses of the HDACi givinostat have been used in children to reduce arthritis and are well tolerated. In addition to the antiinflammatory properties, HDACi's have shown promise in models of neurodegenerative disorders, and HDACi's also hold promise to drive HIV-1 out of latently infected cells. No one molecular mechanism accounts for the non-cancer-related properties of HDACi's, since there are 18 genes coding for histone deacetylases. Rather, there are mechanisms unique for the pathological process of specific cell types. In this overview, we summarize the preclinical data on HDACi's for therapy in a wide spectrum of diseases unrelated to the treatment of cancer. The data suggest the use of HDACi's in treating autoimmune as well as chronic inflammatory diseases.
本期《分子医学》包含了 14 篇关于组蛋白去乙酰化酶抑制剂(HDACi)的原始研究报告和最新综述,这些研究都集中在与促凋亡特性无关的广泛疾病模型中,这些疾病模型与癌症治疗相关。这些疾病对 HDACi 有反应的范围主要归因于其几种抗炎特性,这些特性通常在体外观察到,但在动物模型中也很重要。一个统一的特性是细胞因子产生的减少以及细胞因子受体后信号的抑制。与它们在癌症中的应用不同,HDACi 对炎症的抑制作用在低浓度下就可以观察到,而在杀死肿瘤细胞所需的浓度更高。这一特性使得 HDACi 成为治疗慢性疾病的有吸引力的候选药物,因为低剂量的药物就能耐受。例如,低剂量的口服 HDACi givinostat 已被用于儿童减少关节炎,且耐受性良好。除了抗炎特性,HDACi 在神经退行性疾病模型中也显示出了希望,并且 HDACi 也有望将 HIV-1 从潜伏感染的细胞中清除。没有一个分子机制可以解释 HDACi 与癌症无关的特性,因为有 18 个基因编码组蛋白去乙酰化酶。相反,针对特定细胞类型的病理过程有其独特的机制。在这篇综述中,我们总结了 HDACi 在治疗与癌症治疗无关的广泛疾病中的临床前数据。这些数据表明,HDACi 可用于治疗自身免疫性和慢性炎症性疾病。