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The eIF2-alpha kinase HRI: a potential target beyond the red blood cell

机译：EIF2-α激酶HRI：超出红细胞的潜在目标

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Introduction: The eIF2 kinase heme-regulated inhibitor (HRI) is one of four well-described kinases that phosphorylate eIF2 in response to various cell stressors, resulting in reduced ternary complex formation and attenuation of mRNA translation. Although HRI is well known for its role as a heme sensor in erythroid progenitors, pharmacologic activation of HRI has been demonstrated to have anti-cancer activity across a wide range of tumor sub-types. Here, the potential of HRI activators as novel cancer therapeutics is explored.Areas covered: We provide an introduction to eIF2 signaling pathways in general, and specifically review data on the eIF2 kinase HRI in erythroid and non-erythroid cells. We review aspects of targeting eIF2 signaling in cancer and highlight promising data using HRI activators against tumor cells.Expert opinion: Pharmacologic activation of HRI inhibits tumor growth as a single agent without appreciable toxicity in vivo. The ability of HRI activators to provide direct and sustained eIF2 phosphorylation without inducing oxidative stress or broad eIF2 kinase activation may be especially advantageous for tolerability. Combination therapy with established therapeutics may further augment anti-cancer activity to overcome disease resistance.
机译：介绍：EIF2激酶血红素调节抑制剂（HRI）是磷酸化效果响应于各种细胞应激源的四种富孔的激酶之一，导致三元复合形成和mRNA翻译的衰减。尽管HRI以其作为红细胞祖的血红素传感器的作用而闻名，但HRI的药理学活化已被证明在各种肿瘤子类型中具有抗癌活性。在这里，探讨了作为新型癌症治疗剂的HRI活化剂的潜力。覆盖：我们一般提供EIF2信号传导途径的介绍，具体介绍红细胞和非红细胞细胞的EIF2激酶HRI上的数据。我们审查靶向癌症中的EIF2信号传导的方面，并使用HRI活化剂对抗肿瘤细胞来突出有希望的数据。普及意见：HRI的药理学活化抑制肿瘤生长作为单一剂，而在体内没有明显的毒性。 HRI活化剂在不诱导氧化应激或广泛的EIF2激酶活化的情况下提供直接和持续的EIF2磷酸化的能力可能是特别有利的。结合治疗的治疗方法可能进一步增加抗癌活动以克服抗病抗性。

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