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受体酪氨酸激酶 (RTK)家族是一类具有内源性蛋白酪氨酸激酶 (PTK)活性的单次跨膜受体 ,它们在调控与细胞增殖、分化等相关的信号转导通路中起关键作用。它与配体结合后引起二聚化或结构重排而使胞内区的酪氨酸 (Tyr)被自磷酸化。Tyr的自磷酸化一方面可以激活胞内PTK区的活性 ,另一方面可以为下游的信号蛋白提供结合位点从而完成活化过程。本文对RTK家族成员的晶体结构及其活性调节机制的研究进行了综述 ,阐述了由配体诱导RTK活化的结构基础 ,并简要讨论了RTK抑制剂可能的作用靶点
The receptor tyrosine kinase (RTK) family is a family of single transmembrane receptors with endogenous protein tyrosine kinase (PTK) activity that regulate signaling pathways involved in cell proliferation, differentiation, and the like Play a key role. It binds to the ligand to cause dimerization or structural rearrangement and the intracellular tyrosine (Tyr) is autophosphorylated. Tyr autophosphorylation on the one hand can activate the activity of the intracellular PTK region, on the other hand can provide binding sites for the downstream signal protein in order to complete the activation process. This review summarizes the crystal structure and activity regulation mechanism of RTK family members, elaborates the structural basis of ligand-induced RTK activation and briefly discusses the possible target of RTK inhibitor