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首页> 外文期刊>Expert opinion on therapeutic targets >Emerging strategies for EphA2 receptor targeting for cancer therapeutics.
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Emerging strategies for EphA2 receptor targeting for cancer therapeutics.

机译：EphA2受体靶向治疗癌症的新兴策略。

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IMPORTANCE OF THE FIELD: High mortality rates with cancers warrant further development of earlier diagnostics and better treatment strategies. Membrane-bound erythropoietin-producing hepatocellular receptor tyrosine kinase class A2 (EphA2) is overexpressed in breast, prostate, urinary bladder, skin, lung, ovary and brain cancers. AREAS COVERED IN THIS REVIEW: EphA2 overexpression in cancers, its signaling mechanisms and strategies to target its deregulation. WHAT THE READER WILL GAIN: High EphA2 expression in cancer cells is correlated with a poor prognosis associated with recurrence due to enhanced metastasis. Interaction of the EphA2 receptor with its ligand (e.g., ephrinA1) triggers events that are deregulated and implicated in carcinogenesis. EphrinA1-independent oncogenic activity and ephrinA1-dependent tumor suppressor roles for EphA2 are described. Molecular interactions of EphA2 with signaling proteins are associated with the modulation of cytoskeleton dynamics, cell adhesion, proliferation, differentiation and metastasis. The deregulated signaling by EphA2 and its involvement in oncogenesis provide multiple avenues for the rational design of intervention approaches. TAKE HOME MESSAGE: EphA2 has been tested as a drug target using multiple approaches such as agonist antibodies, RNA interference, immunotherapy, virus vector-mediated gene transfer, small-molecule inhibitors and nanoparticles. With over a decade of research, encouraging results with targeting of EphA2 expression in various pre-clinical cancer models necessitate further studies.
机译：领域的重要性：癌症的高死亡率保证了早期诊断方法和更好治疗策略的进一步发展。在乳腺癌，前列腺癌，膀胱癌，皮肤癌，肺癌，卵巢癌和脑癌中过表达膜结合型促红细胞生成素的肝细胞受体酪氨酸激酶A2（EphA2）过表达。这篇综述涵盖的领域：EphA2在癌症中的过度表达，其信号传导机制和针对其放松调节的策略。读者将会收获什么：癌细胞中高EphA2表达与由于转移增加而复发相关的不良预后相关。 EphA2受体与其配体（例如ephrinA1）的相互作用触发了被放松调节并参与致癌作用的事件。描述了EphA2的依赖于EphrinA1的致癌活性和依赖ephrinA1的肿瘤抑制因子。 EphA2与信号蛋白的分子相互作用与细胞骨架动力学，细胞粘附，增殖，分化和转移的调节有关。 EphA2解除了信号转导，并参与了肿瘤发生，为合理设计干预方法提供了多种途径。温馨提示：EphA2已通过多种方法测试为药物靶标，例如激动剂抗体，RNA干扰，免疫疗法，病毒载体介导的基因转移，小分子抑制剂和纳米颗粒。经过十多年的研究，在各种临床前癌症模型中靶向EphA2表达的令人鼓舞的结果需要进一步的研究。

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