Metals Biology and Molecular Medicine Group, Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD), and.
Veterinary Resources Program, NIH, Bethesda, Maryland, USA.
J Clin Invest. 2018 Apr 2;128(4):1317-1325. doi: 10.1172/JCI97684. Epub 2018 Feb 26.
Chuvash polycythemia is an inherited disease caused by a homozygous germline VHLR200W mutation, which leads to impaired degradation of HIF2α, elevated levels of serum erythropoietin, and erythrocytosis/polycythemia. This phenotype is recapitulated by a mouse model bearing a homozygous VhlR200W mutation. We previously showed that iron-regulatory protein 1-knockout (Irp1-knockout) mice developed erythrocytosis/polycythemia through translational derepression of Hif2α, suggesting that IRP1 could be a therapeutic target to treat Chuvash polycythemia. Here, we fed VhlR200W mice supplemented with Tempol, a small, stable nitroxide molecule and observed that Tempol decreased erythropoietin production, corrected splenomegaly, normalized hematocrit levels, and increased the lifespans of these mice. We attribute the reversal of erythrocytosis/polycythemia to translational repression of Hif2α expression by Tempol-mediated increases in the IRE-binding activity of Irp1, as reversal of polycythemia was abrogated in VhlR200W mice in which Irp1 was genetically ablated. Thus, a new approach to the treatment of patients with Chuvash polycythemia may include dietary supplementation of Tempol, which decreased Hif2α expression and markedly reduced life-threatening erythrocytosis/polycythemia in the VhlR200W mice.
楚瓦什红细胞增多症是一种遗传性疾病,由同源性胚系 VHLR200W 突变引起,导致 HIF2α 降解受损、血清促红细胞生成素水平升高以及红细胞增多/红细胞增多症。这种表型在携带同源性 VhlR200W 突变的小鼠模型中得到重现。我们之前曾表明,铁调节蛋白 1 敲除(Irp1-knockout)小鼠通过 Hif2α 的翻译去抑制发展为红细胞增多/红细胞增多症,表明 IRP1 可能是治疗楚瓦什红细胞增多症的治疗靶点。在这里,我们给 VhlR200W 小鼠喂食了 Tempol,一种小型、稳定的氮氧化物分子,观察到 Tempol 降低了促红细胞生成素的产生,纠正了脾肿大,使红细胞比容水平正常化,并延长了这些小鼠的寿命。我们将红细胞增多/红细胞增多症的逆转归因于 Tempol 介导的 Irp1 的 IRE 结合活性增加,从而抑制了 Hif2α 的表达,因为在 Irp1 基因敲除的 VhlR200W 小鼠中,红细胞增多症的逆转被阻断。因此,治疗楚瓦什红细胞增多症患者的新方法可能包括 Tempol 的饮食补充,它降低了 Hif2α 的表达,并显著减少了 VhlR200W 小鼠危及生命的红细胞增多/红细胞增多症。