Department of Medical Oncology & Therapeutics Research, City of Hope National Medical Center, 1500 East Duarte Road, Duarte, CA, United States.
Department of Medical Oncology & Therapeutics Research, City of Hope National Medical Center, 1500 East Duarte Road, Duarte, CA, United States.
Biochim Biophys Acta Rev Cancer. 2018 Apr;1869(2):128-137. doi: 10.1016/j.bbcan.2018.01.003. Epub 2018 Jan 31.
The erythropoietin-producing hepatocellular carcinoma (Eph) receptors are the largest family of receptor tyrosine kinases (RTKs) that include two major subclasses, EphA and EphB. They form an important cell communication system with critical and diverse roles in a variety of biological processes during embryonic development. However, dysregulation of the Eph/ephrin interactions is implicated in cancer contributing to tumour growth, metastasis, and angiogenesis. Here, we focus on EphB4 and review recent developments in elucidating its role in upper aerodigestive malignancies to include lung cancer, head and neck cancer, and mesothelioma. In particular, we summarize information regarding EphB4 structure/function and role in disease pathobiology. We also review the data supporting EphB4 as a potential pharmacological and immunotherapy target and finally, progress in the development of new therapeutic strategies including small molecule inhibitors of its activity is discussed. The emerging picture suggests that EphB4 is a valuable and attractive therapeutic target for upper aerodigestive malignancies.
促红细胞生成素产生的肝细胞癌 (Eph) 受体是受体酪氨酸激酶 (RTK) 家族中最大的家族,包括两个主要亚类,EphA 和 EphB。它们形成了一个重要的细胞通讯系统,在胚胎发育过程中的多种生物学过程中具有关键和多样化的作用。然而,Eph/ephrin 相互作用的失调与肿瘤的发生有关,有助于肿瘤生长、转移和血管生成。在这里,我们重点关注 EphB4,并回顾了最近在阐明其在上呼吸道恶性肿瘤中的作用方面的进展,包括肺癌、头颈部癌和间皮瘤。特别是,我们总结了 EphB4 的结构/功能及其在疾病病理生物学中的作用的信息。我们还回顾了支持 EphB4 作为潜在的药理学和免疫治疗靶点的数据,最后讨论了其活性的小分子抑制剂等新治疗策略的进展。新兴的研究表明,EphB4 是上呼吸道恶性肿瘤的一个有价值和有吸引力的治疗靶点。