选择性PI3Kδ抑制剂的研究进展

Advances in PI3Kδ selective inhibitors

磷脂酰肌醇3-激酶(phosphoinositide 3-kinase,PI3K)是PI3K/AKT/m TOR信号通路中的关键调节激酶,属于脂激酶家族成员,参与调控细胞的增殖、分化、凋亡以及血管生成过程。PI3K异常激活与多种肿瘤的发生发展密切相关。PI3Kδ(PI3K delta)是PI3K激酶的一种亚型,主要存在于免疫细胞和血液细胞中。近年来针对PI3Kδ亚型开发选择性PI3Kδ抑制剂用于血液肿瘤的治疗备受关注。本文综述了选择性PI3Kδ抑制剂的研究进展,为合理开发选择性PI3Kδ抑制剂提供启示。

Phosphoinositide 3-kinase （ PI3K）, a key regulator in the PI3K/AKT/mTOR signaling pathway, plays a critical role in regulation of cell growth, differentiation, metastasis apoptosis, and angiogenesis proces- ses. Abnormal activation of PI3K is closely related to the development of many types of human cancers. PI3Kδ is an important isoform of PI3K family, mainly expressed in leukocytes, which makes it an attractive target for the treatment of hematological malignancies. Great efforts in both industry and academia have been made to develop PI3 Kδ selective inhibitors as anti-cancer agents. This review attempts to provide an overview of recent advances in the research of PI3Kδ selective inhibitors, fueling the progress of the ideal selective PI3Kδ inhibitors in the future.