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磷脂酰肌醇3-激酶(PI3K)是一类脂质与蛋白激酶家族,其主要通过在磷脂酰肌醇的肌醇环三位进行磷酸化产生胞内重要的第二信使——磷脂酰肌醇-3,4,5-三磷酸(phosphatidyl inositol 3,4,5-trisphosphate,PIP3)而发挥作用.磷脂酰肌醇3-激酶γ/δ(PI3Kγ/δ)是I类PI3K家族中的成员,其主要表达于免疫相关细胞中,这2种PI3K亚型参与先天性与获得性免疫应答.因此,PI3Kγ/PI3Kδ被视为因免疫反应调控异常导致的炎症疾病的治疗药物靶点.目前,利用特异性抑制剂靶向干预PI3Kγ和/或PI3Kδ,成为炎症相关疾病治疗的新策略.本文简介了PI3Kγ与PI3Kδ在不同类型免疫细胞中的功能;并就采用小分子特异性抑制剂,靶向抑制PI3Kγ和/或PI3Kδ在各类炎症相关疾病中的治疗作用和效果进行综述.
Phosphatidylinositol 3-kinases (PI3Ks) are a family of lipid and protein kinases that are primarily phosphorylated by phosphorylation at the 3 ’position of the inositol ring of phosphatidylinositol to produce the intracellularly important second messenger phosphatidylinositol Phosphatidylinositol 3,4,5-trisphosphate (PIP3) .Phosphatidylinositol 3-kinase γ / δ (PI3Kγ / δ) is a member of the class I PI3K family , Which is mainly expressed in immune-related cells, which are involved in both innate and adaptive immune responses.Therefore, PI3Kγ / PI3Kδis regarded as a therapeutic drug target for inflammatory diseases caused by abnormal immune regulation.At present, Targeted intervention of PI3Kγ and / or PI3Kδ with specific inhibitors has become a new strategy for the treatment of inflammation-related diseases.In this paper, the functions of PI3Kγ and PI3Kδ in different types of immune cells are briefly introduced. In addition, the use of small molecule-specific inhibitors Therapeutic effects and effects of inhibiting PI3Kγ and / or PI3Kδ in various types of inflammation-related diseases are reviewed.