巨噬细胞集落刺激因子受体激酶及其抑制剂的研究进展

Macrophage colony-stimulating factor receptor and its inhibitors: research advances

巨噬细胞集落刺激因子受体(c-Fms)是原癌基因c-fms的编码产物,属于Ⅲ型受体酪氨酸激酶家族成员。巨噬细胞集落刺激因子与c-Fms结合,激活其酪氨酸激酶,在单核巨噬细胞系的存活、增殖、分化以及胚胎发育过程中发挥着重要的作用。c-Fms及其配体的过度表达,引起该受体介导的细胞信号通路异常激活,参与了肿瘤形成和炎症发生过程。因此,靶向c-Fms激酶的抑制剂能抑制受体的磷酸化,阻断受体介导的细胞信号通路,是治疗肿瘤、关节炎等疾病的潜在药物。

Macrophage colony-stimulating factor receptor（c-Fms）,encoded by the c-fms proto-oncogene,is a member of type Ⅲ receptor tyrosine kinase family. c-Fms activation by binding with its ligand plays important roles in the survival, proliferation and differentiation of the monocyte-macrophage lineage and the development of embryo. Over expression of c-Fms and its ligand result in abnormalities of intracellular signaling pathways mediated by c-Fms, which is associated with tumorigenesis and inflammation. The inhibitors targeting c-Fms block intracellular signaling pathways by inhibiting c-Fms receptor tyrosine kinase are potential drugs for tumor and arthritis therapeutics.