2. 重组蛋白
  3. Cytokines and Growth Factors
  4. Ephrin/Eph Family

Ephrin/Eph Family  (Ephrin 家族)

Ephrins是一类与 Eph 受体结合的配体，Eph 受体是酪氨酸激酶受体中最大的一个家族。Ephrins和Eph家族是膜结合分子，通过细胞-细胞接触介导短期轴突导向。Ephrins 可分为两大类，一种是通过糖基磷脂酰肌醇 (GPI) 部分连接到细胞膜上的ephrinAs (A1-A6)，另一种是跨越细胞膜并拥有细胞质信号域的ephrinBs (B1-B3)。在人类基因组中，共有9个EphA 受体和5个EphB受体。EphA 受体混杂地结合5个Ephrin-A配体，EphB 受体混杂地结合3个Ephrin-B配体。Eph/Ephrin信号转导是双向的，在 Eph 受体表达细胞中称为正向信号转导，在 Ephrin 配体表达细胞中称为反向信号转导。Eph/Ephrin信号通路在发育过程、成体组织稳态和各种疾病中发挥重要作用，它的异常功能与包括癌症在内的各种疾病有关。鉴于Eph受体及其配体在人类恶性肿瘤中常过表达并与不良预后相关，Eph受体和Ephrins被认为是非常有前途的药物靶点。

Ephrins are a family of ligands that bind to the Eph receptors, the largest family of receptor tyrosine kinases. Ephrins and the Eph family are membrane-bound molecules that mediate short-range axon guidance via cell-cell contacts. The ephrins fall into two broad classes, the ephrinAs (ephrins A1-A6), which are attached to the cell membrane by a glycosyl phosphatidylinositol (GPI) moiety, and the ephrinBs (ephrins B1-B3), which span the cellular membrane and possess a cytoplasmic signaling domain. In the human genome, there are totally nine EphA and five EphB receptors. The EphA receptors promiscuously bind to five Ephrin-A ligands, and the EphB receptors promiscuously bind three Ephrin-B ligands. Ephrin-Eph signaling is bidirectional which is termed forward signaling in Eph receptor-expressing cells and reverse signaling in ephrin ligand-expressing cells. The Eph/ephrin signaling plays important roles in developmental processes, adult tissue homeostasis and various diseases. Its abnormal function has been implicated in various diseases, including cancer. Given Eph receptors and Ephrins are often overexpressed in human malignancies and associated with poor prognosis, they are considered as very promising drug targets.

 
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