Department of Medicine, Virginia Commonwealth University Health Systems, Richmond, VA 23298, USA.
Blood. 2010 Jun 3;115(22):4478-87. doi: 10.1182/blood-2009-12-257261. Epub 2010 Mar 16.
Interactions between histone deacetylase inhibitors (HDACIs) and the novel proteasome inhibitor carfilzomib (CFZ) were investigated in GC- and activated B-cell-like diffuse large B-cell lymphoma (ABC-DLBCL) cells. Coadministration of subtoxic or minimally toxic concentrations of CFZ) with marginally lethal concentrations of HDACIs (vorinostat, SNDX-275, or SBHA) synergistically increased mitochondrial injury, caspase activation, and apoptosis in both GC- and ABC-DLBCL cells. These events were associated with Jun NH2-terminal kinase (JNK) and p38MAPK activation, abrogation of HDACI-mediated nuclear factor-kappaB activation, AKT inactivation, Ku70 acetylation, and induction of gammaH2A.X. Genetic or pharmacologic JNK inhibition significantly diminished CFZ/vorinostat lethality. CFZ/vorinostat induced pronounced lethality in 3 primary DLBCL specimens but minimally affected normal CD34(+) hematopoietic cells. Bortezomib-resistant GC (SUDHL16) and ABC (OCI-LY10) cells exhibited partial cross-resistance to CFZ. However, CFZ/vorinostat dramatically induced resistant cell apoptosis, accompanied by increased JNK activation and gammaH2A.X expression. Finally, subeffective vorinostat doses markedly increased CFZ-mediated tumor growth suppression and apoptosis in a murine xenograft OCI-LY10 model. These findings indicate that HDACIs increase CFZ activity in GC- and ABC-DLBCL cells sensitive or resistant to bortezomib through a JNK-dependent mechanism in association with DNA damage and inhibition of nuclear factor-kappaB activation. Together, they support further investigation of strategies combining CFZ and HDACIs in DLBCL.
组蛋白去乙酰化酶抑制剂 (HDACIs) 与新型蛋白酶体抑制剂卡非佐米 (CFZ) 之间的相互作用在 GC- 和激活 B 细胞样弥漫性大 B 细胞淋巴瘤 (ABC-DLBCL) 细胞中进行了研究。在 GC- 和 ABC-DLBCL 细胞中,亚毒性或最小毒性浓度的 CFZ 与边缘致死浓度的 HDACIs(伏立诺他、SNDX-275 或 SBHA)联合给药可协同增加线粒体损伤、半胱天冬酶激活和细胞凋亡。这些事件与 Jun NH2-末端激酶 (JNK) 和 p38MAPK 激活、阻断 HDACI 介导的核因子-κB 激活、AKT 失活、Ku70 乙酰化和诱导 γH2A.X 有关。遗传或药理学 JNK 抑制显著降低了 CFZ/伏立诺他的致死率。CFZ/伏立诺他在 3 个原发性 DLBCL 标本中引起明显的致死性,但对正常 CD34(+) 造血细胞的影响很小。硼替佐米耐药的 GC(SUDHL16)和 ABC(OCI-LY10)细胞对 CFZ 表现出部分交叉耐药性。然而,CFZ/伏立诺他显著诱导耐药细胞凋亡,同时伴有 JNK 激活和 γH2A.X 表达增加。最后,亚效剂量的伏立诺他显著增加了 CFZ 在小鼠异种移植 OCI-LY10 模型中对肿瘤生长的抑制作用和细胞凋亡。这些发现表明,HDACIs 通过一种与 DNA 损伤和核因子-κB 激活抑制相关的 JNK 依赖性机制,增加 GC- 和 ABC-DLBCL 细胞对硼替佐米敏感或耐药的 CFZ 活性。综上所述,它们支持进一步研究 CFZ 和 HDACIs 联合治疗 DLBCL 的策略。