雷帕霉素的免疫药理学（综述）

雷帕霉素是一种高效低毒的大环内酯类免疫抑制药，它在细胞外的受体为FK506结合蛋白FKBP－12，胞浆内的激酶mTOR是雷帕霉素已知的主要靶体，它是mRNA翻译的启动调控因子，Kipl是一种周期素依赖性激酶的抑制剂，能降低活化的T细胞内G1期的周期素与其依赖性激酶复合物的水平，mTOR对p70 s6k的活性，真核启努因子4E依赖性蛋白合成及Kip1的下调所需调节信号具有诱变作用，它与FKBP12与雷帕霉素复合物的相互作用干扰了它的功能，雷帕霉素因素阻断了Kipl的下调而将细胞阻滞于G1期。

Immunopharmacology of rapamycin (A review)

Rapamycin is a macrolide with strong immunosuppressive activity and lower toxicity. Its in-tracellular receptor is the FK506 binding protein (FKBP- 12). The cytosolic kinase mTOR which con-trols the initiation of the translation of messenger RNA is the main known target of rapamycin. Kip1 is acyclin-dependent kinase inhibitor, which can reduce the G1-cyclin-cdk complexes in activated Tcells. The mTOR fimctions as an inducible transducer of regulatory signals for p70S6K activation, eukary-otic initiation factor 4E-dependent protein synthesis, and Kip1 downregulation. Interaction of mTORwith FKBP12*rapamycin disrupts mTOR-dependent functions. So that, rapamycin inhibits C1-phaseprogression by blocking Kip1 downregulation.