脂类磷脂酰肌醇是几乎所有细胞生死的主要调节因子，是由磷脂酰肌醇激酶的紧密调节活动所产生的。尽管长期以来一直致力于研究I类磷脂酰肌醇3激酶 (PI3Ks)的药物作用，但近年来发现了针对几乎所有人类疾病中的磷脂酰肌醇激酶的机会，包括癌症、免疫缺陷、病毒感染和神经退行性疾病。这导致广泛的努力在临床开发磷脂酰肌醇激酶的有效和选择性抑制剂。本综述总结了磷脂酰肌醇激酶在疾病中参与的分子基础，并评估了磷脂酰肌醇激酶抑制剂的临床前和临床发展进展。 © 2022 年 Springer Nature Limited。

Lipid phosphoinositides are master regulators of almost all aspects of a cell's life and death and are generated by the tightly regulated activity of phosphoinositide kinases. Although extensive efforts have focused on drugging class I phosphoinositide 3-kinases (PI3Ks), recent years have revealed opportunities for targeting almost all phosphoinositide kinases in human diseases, including cancer, immunodeficiencies, viral infection and neurodegenerative disease. This has led to widespread efforts in the clinical development of potent and selective inhibitors of phosphoinositide kinases. This Review summarizes our current understanding of the molecular basis for the involvement of phosphoinositide kinases in disease and assesses the preclinical and clinical development of phosphoinositide kinase inhibitors.© 2022. Springer Nature Limited.