Research progress of phosphatidylinositol 4-kinase and its inhibitors in inflammatory diseases
Research progress of phosphatidylinositol 4-kinase and its inhibitors in inflammatory diseases
复制标题
磷脂酰肌醇4-激酶及其抑制剂在炎症性疾病中的研究进展
DOI：
10.1016/j.ejphar.2021.174300
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发表时间：
2021-07-06
影响因子：
5
通讯作者：
Xu, Ming
中科院分区：
文献类型：
--
作者：
Li, Yan-ping;Mikrani, Reyaj;Xu, Ming
磷脂酰肌醇4-激酶（PI4K）是一种脂质激酶，可以催化磷酸基团从ATP转移到磷脂酰肌醇（PtdIns）的肌醇环上，导致PtdIns在4-OH位点磷酸化，生成磷脂酰肌醇4-磷酸（PI4P）。生物学功能研究表明，PI4K与肥胖、癌症、病毒感染、疟疾、阿尔茨海默病等多种炎性疾病的发生发展密切相关。pi4k相关抑制剂已被发现在器官移植中具有抑制病毒复制、抗癌、治疗疟疾和减少排斥反应的作用，其中抗疟疾药物MMV390048已进入II期临床试验。本文综述了PI4K的分类、结构、分布和相关抑制剂及其在癌症、病毒复制和其他炎症诱导疾病进展中的作用，以探索其作为治疗靶点的潜力。
Phosphatidylinositol 4-kinase (PI4K) is a lipid kinase that can catalyze the transfer of phosphate group from ATP to the inositol ring of phosphatidylinositol (PtdIns) resulting in the phosphorylation of PtdIns at 4-OH sites, to generate phosphatidylinositol 4-phosphate (PI4P). Studies on biological functions reveal that PI4K is closely related to the occurrence and development of various inflammatory diseases such as obesity, cancer, viral infections, malaria, Alzheimer's disease, etc. PI4K-related inhibitors have been found to have the effects of inhibiting virus replication, anti-cancer, treating malaria and reducing rejection in organ transplants, among which MMV390048, an anti-malaria drug, has entered phase II clinical trial. This review discusses the classification, structure, distribution and related inhibitors of PI4K and their role in the progression of cancer, viral replication, and other inflammation induced diseases to explore their potential as therapeutic targets.