Baudet Sarah, Bécret Johann, Nicol Xavier
Institut de la Vision, Sorbonne Université, Inserm, CNRS, 17 rue Moreau, F-75012 Paris, France.
Pharmaceuticals (Basel). 2020 Jun 30;13(7):140. doi: 10.3390/ph13070140.
Erythropoietin-producing hepatocellular carcinoma A (EphA) receptors and their ephrin-A ligands are key players of developmental events shaping the mature organism. Their expression is mostly restricted to stem cell niches in adults but is reactivated in pathological conditions including lesions in the heart, lung, or nervous system. They are also often misregulated in tumors. A wide range of molecular tools enabling the manipulation of the ephrin-A:EphA system are available, ranging from small molecules to peptides and genetically-encoded strategies. Their mechanism is either direct, targeting EphA receptors, or indirect through the modification of intracellular downstream pathways. Approaches enabling manipulation of ephrin-A:EphA forward signaling for the dissection of its signaling cascade, the investigation of its physiological roles or the development of therapeutic strategies are summarized here.
促红细胞生成素产生性肝细胞癌A（EphA）受体及其Ephrin-A配体是塑造成熟生物体发育事件的关键参与者。它们的表达在成年人中大多局限于干细胞龛，但在包括心脏、肺或神经系统病变在内的病理条件下会重新激活。它们在肿瘤中也常常调控异常。现在有各种各样的分子工具可用于操控Ephrin-A：EphA系统，从小分子到肽以及基因编码策略都有。它们的作用机制要么是直接靶向EphA受体，要么是通过修饰细胞内下游途径间接发挥作用。本文总结了能够操控Ephrin-A：EphA正向信号传导以剖析其信号级联、研究其生理作用或开发治疗策略的方法。
