Zozulya S A, Udovichenko I P
Bioorg Khim. 2012 May-Jun;38(3):267-79. doi: 10.1134/s106816201203017x.
Anti-angiogenic therapy is currently a commonly accepted and rapidly developing approach in oncology and other pathologies linked to aberrant neovascularization. Discovery and validation of additional molecular targets in angiogenesis is needed due to the limitations of the existing clinical therapeutics inhibiting activity of vascular endothelial growth factor (VEGF) and its receptors. A brief review of normal and pathological biological functions of the Eph family of receptor tyrosine kinases and their ephrin ligands is presented, and the approaches to developing therapeutics with anti- and pro-angiogenic and anti-tumor activity based on selective molecular modulation of Eph-ephrin signaling pairs are discussed. Functional roles of Eph-kinases and ephrins in such mechanisms of cancerogenesis as cell proliferation and invasion are also addressed.
抗血管生成疗法目前是肿瘤学以及与异常血管生成相关的其他病理学中一种普遍接受且快速发展的方法。由于现有临床治疗方法在抑制血管内皮生长因子(VEGF)及其受体活性方面存在局限性,因此需要发现并验证血管生成中的其他分子靶点。本文简要综述了受体酪氨酸激酶Eph家族及其 Ephrin 配体的正常和病理生物学功能,并讨论了基于对 Eph-Ephrin 信号对进行选择性分子调节来开发具有抗血管生成、促血管生成和抗肿瘤活性的治疗方法。还探讨了 Eph 激酶和 Ephrins 在细胞增殖和侵袭等癌症发生机制中的功能作用。