Clinical Research Institute, Zhejiang Provincial People's Hospital, Hangzhou, 310014, Zhejiang, China.
College of Pharmaceutical Sciences, Soochow University, Suzhou 215123, China.
Curr Protein Pept Sci. 2024;25(3):244-255. doi: 10.2174/0113892037269589231017055642.
Eph receptors and their Eph receptor-interacting (ephrin) ligands comprise a vital cell communication system with several functions. In cancer cells, there was evidence of bilateral Eph receptor signaling with both tumor-suppressing and tumor-promoting actions. As a member of the Eph receptor family, EphB4 has been linked to tumor angiogenesis, growth, and metastasis, which makes it a viable and desirable target for drug development in therapeutic applications. Many investigations have been conducted over the last decade to elucidate the structure and function of EphB4 in association with its ligand ephrinB2 for its involvement in tumorigenesis. Although several EphB4-targeting drugs have been investigated, and some selective inhibitors have been evaluated in clinical trials. This article addresses the structure and function of the EphB4 receptor, analyses its possibility as an anticancer therapeutic target, and summarises knowledge of EphB4 kinase inhibitors. To summarise, EphB4 is a difficult but potential treatment option for cancers.
Eph 受体及其 Eph 受体相互作用（ephrin）配体构成了一个重要的细胞通讯系统，具有多种功能。在癌细胞中，有证据表明 Eph 受体信号具有双向作用，既有抑制肿瘤的作用，也有促进肿瘤的作用。作为 Eph 受体家族的一员，EphB4 与肿瘤血管生成、生长和转移有关，使其成为治疗应用中药物开发的可行和理想靶点。在过去的十年中，已经进行了许多研究来阐明 EphB4 与其配体 EphrinB2 相关的结构和功能，以研究其在肿瘤发生中的作用。尽管已经研究了几种 EphB4 靶向药物，并且已经在临床试验中评估了一些选择性抑制剂，但本文将讨论 EphB4 受体的结构和功能，分析其作为抗癌治疗靶点的可能性，并总结 EphB4 激酶抑制剂的知识。总之，EphB4 是癌症治疗的一个困难但有潜力的选择。
