Division of Radioprotectants, Department of Pharmacology and Molecular Therapeutics, F. Edward Hébert School of Medicine, Uniformed Services University of the Health Sciences, Bethesda, Maryland 20814, United States.
Armed Forces Radiobiology Research Institute, Uniformed Services University of the Health Sciences, Bethesda, Maryland 20814, United States.
J Proteome Res. 2023 Apr 7;22(4):1116-1126. doi: 10.1021/acs.jproteome.2c00458. Epub 2023 Mar 28.
There are currently four radiation medical countermeasures that have been approved by the United States Food and Drug Administration to mitigate hematopoietic acute radiation syndrome, all of which are repurposed radiomitigators. The evaluation of additional candidate drugs that may also be helpful for use during a radiological/nuclear emergency is ongoing. A chlorobenzyl sulfone derivative (organosulfur compound) known as Ex-Rad, or ON01210, is one such candidate medical countermeasure, being a novel, small-molecule kinase inhibitor that has demonstrated efficacy in the murine model. In this study, nonhuman primates exposed to ionizing radiation were subsequently administered Ex-Rad as two treatment schedules (Ex-Rad I administered 24 and 36 h post-irradiation, and Ex-Rad II administered 48 and 60 h post-irradiation) and the proteomic profiles of serum using a global molecular profiling approach were assessed. We observed that administration of Ex-Rad post-irradiation is capable of mitigating radiation-induced perturbations in protein abundance, particularly in restoring protein homeostasis, immune response, and mitigating hematopoietic damage, at least in part after acute exposure. Taken together, restoration of functionally significant pathway perturbations may serve to protect damage to vital organs and provide long-term survival benefits to the afflicted population.
目前,有四种辐射医学对策已被美国食品和药物管理局批准用于减轻造血急性辐射综合征,它们都是重新利用的辐射缓解剂。正在对可能在放射性/核紧急情况下也有帮助的其他候选药物进行评估。一种名为 Ex-Rad(或 ON01210)的氯苄基砜衍生物(有机硫化合物)就是这样一种候选医学对策,它是一种新型小分子激酶抑制剂,在小鼠模型中已显示出疗效。在这项研究中,随后用两种治疗方案(Ex-Rad I 在辐照后 24 和 36 小时给药,Ex-Rad II 在辐照后 48 和 60 小时给药)给暴露于电离辐射的非人类灵长类动物施用 Ex-Rad,并使用全局分子分析方法评估血清的蛋白质组谱。我们观察到,辐照后给予 Ex-Rad 能够减轻辐射引起的蛋白质丰度变化,特别是在恢复蛋白质平衡、免疫反应和减轻造血损伤方面,至少在急性暴露后部分如此。总之,功能重要的途径变化的恢复可能有助于保护重要器官免受损伤,并为受影响的人群提供长期生存益处。