Department of Microbiology, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.
Department of Microbiology, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.
Antiviral Res. 2021 Sep;193:105124. doi: 10.1016/j.antiviral.2021.105124. Epub 2021 Jun 28.
Human cytomegalovirus (HCMV) is a ubiquitous pathogen that establishes a life-long infection affecting up to 80% of the US population. HCMV periodically reactivates leading to enhanced morbidity and mortality in immunosuppressed patients causing a range of complications including organ transplant failure and cognitive disorders in neonates. Therapeutic options for HCMV are limited to a handful of antivirals that target late stages of the virus life cycle and efficacy is often challenged by the emergence of mutations that confer resistance. In addition, these antiviral therapies may have adverse reactions including neutropenia in newborns and an increase in adverse cardiac events in HSCT patients. These findings highlight the need to develop novel therapeutics that target different steps of the viral life cycle. To this end, we screened a small molecule library against ion transporters to identify new antivirals against the early steps of virus infection. We identified valspodar, a 2nd-generation ABC transporter inhibitor, that limits HCMV infection as demonstrated by the decrease in IE2 expression of virus infected cells. Cells treated with increasing concentrations of valspodar over a 9-day period show minimal cytotoxicity. Importantly, valspodar limits HCMV plaque numbers in comparison to DMSO controls demonstrating its ability to inhibit viral dissemination. Collectively, valspodar represents a potential new anti-HCMV therapeutic that limits virus infection by likely targeting a host factor. Further, the data suggest that specific ABC transporters may participate in the HCMV life-cycle.
人巨细胞病毒(HCMV)是一种普遍存在的病原体,可导致终身感染,影响美国 80%以上的人口。HCMV 会周期性地重新激活,导致免疫抑制患者的发病率和死亡率增加,导致一系列并发症,包括器官移植失败和新生儿认知障碍。HCMV 的治疗选择仅限于少数几种靶向病毒生命周期晚期的抗病毒药物,而疗效往往受到导致耐药性的突变的挑战。此外,这些抗病毒疗法可能会产生不良反应,包括新生儿中性粒细胞减少和 HSCT 患者不良心脏事件的增加。这些发现强调需要开发针对病毒生命周期不同步骤的新型治疗方法。为此,我们针对离子转运体筛选了小分子文库,以鉴定针对病毒感染早期步骤的新抗病毒药物。我们发现了 valspodar,一种第二代 ABC 转运体抑制剂,可降低病毒感染细胞中 IE2 的表达,从而限制 HCMV 感染。用递增浓度的 valspodar 处理细胞 9 天,显示出最小的细胞毒性。重要的是,与 DMSO 对照相比,valspodar 限制了 HCMV 斑块数量,证明其抑制病毒传播的能力。总之,valspodar 代表了一种潜在的新型抗 HCMV 治疗药物,通过可能靶向宿主因子来限制病毒感染。此外,数据表明特定的 ABC 转运体可能参与 HCMV 的生命周期。