Department of Medicine, The University of Alabama at Birmingham, Birmingham, Alabama, USA.
J Virol. 2012 Sep;86(17):9055-69. doi: 10.1128/JVI.00793-12. Epub 2012 Jun 13.
Reactivation of latent HIV-1 infection is considered our best therapeutic means to eliminate the latent HIV-1 reservoir. Past therapeutic attempts to systemically trigger HIV-1 reactivation using single drugs were unsuccessful. We thus sought to identify drug combinations consisting of one component that would lower the HIV-1 reactivation threshold and a synergistic activator. With aclacinomycin and dactinomycin, we initially identified two FDA-approved drugs that primed latent HIV-1 infection in T cell lines and in primary T cells for reactivation and facilitated complete reactivation at the population level. This effect was correlated not with the reported primary drug effects but with the cell-differentiating capacity of the drugs. We thus tested other cell-differentiating drugs/compounds such as cytarabine and aphidicolin and found that they also primed latent HIV-1 infection for reactivation. This finding extends the therapeutic promise of N'-N'-hexamethylene-bisacetamide (HMBA), another cell-differentiating agent that has been reported to trigger HIV-1 reactivation, into the group of FDA-approved drugs. To this end, it is also noteworthy that suberoylanilide hydroxamic acid (SAHA), a polar compound that was initially developed as a second-generation cell-differentiating agent using HMBA as a structural template and which is now marketed as the histone deacetylase (HDAC) inhibitor vorinostat, also has been reported to trigger HIV-1 reactivation. Our findings suggest that drugs with primary or secondary cell-differentiating capacity should be revisited as HIV-1-reactivating agents as some could potentially be repositioned as candidate drugs to be included in an induction therapy to trigger HIV-1 reactivation.
潜伏的 HIV-1 感染的激活被认为是消除潜伏 HIV-1 储存库的最佳治疗手段。过去,使用单一药物系统地触发 HIV-1 再激活的治疗尝试都没有成功。因此,我们试图确定由一种降低 HIV-1 再激活阈值的成分和一种协同激活剂组成的药物组合。我们最初使用阿克拉霉素和放线菌素 D 确定了两种 FDA 批准的药物,它们可以激活 T 细胞系和原代 T 细胞中的潜伏 HIV-1 感染,促进群体水平的完全再激活。这种作用与报告的主要药物作用无关,而是与药物的细胞分化能力有关。因此,我们测试了其他具有细胞分化能力的药物/化合物,如阿糖胞苷和阿非迪霉素,发现它们也能引发潜伏 HIV-1 感染的再激活。这一发现将另一种细胞分化剂 N'-N'-己二亚甲基双乙酰酰胺(HMBA)的治疗潜力扩展到 FDA 批准药物的范围。为此,值得注意的是,琥珀酰亚胺基羟肟酸(SAHA)是一种极性化合物,最初是作为第二代细胞分化剂开发的,使用 HMBA 作为结构模板,现在以组蛋白去乙酰化酶(HDAC)抑制剂伏立诺他的形式上市,也被报道可以触发 HIV-1 再激活。我们的发现表明,具有初级或次级细胞分化能力的药物应重新作为 HIV-1 再激活剂进行研究,因为其中一些药物可能具有重新定位的潜力,作为候选药物,包含在诱导治疗中以触发 HIV-1 再激活。