《生命科学》 2014, 26(7): 679-689

IA型磷脂酰肌醇3-激酶与肿瘤的关系及其抑制剂分子机制研究进展

李　玥¹，毛伟峰²，张玉彬^1*

(1 中国药科大学生命科学与技术学院，南京 211198；2 药明康德新药开发有限公司，上海 200131)

摘　要：摘　要：磷脂酰肌醇3- 激酶(phosphatidylinositol-3 kinase， PI3K) 是细胞内重要的信号分子，它具有调节细胞增殖、分化、代谢、凋亡等功能。PI3K 的基因易发生突变和扩增，从而导致PI3K 被激活，与肿瘤的形成和发展密切相关。IA 型的PI3K 及其下游的信号分子组成的通路参与调节肿瘤细胞的增殖、存活、黏附、迁移等活动。综述了IA 型PI3K—— PI3Kα、PI3Kβ 和PI3Kδ 与肿瘤发生、发展的关系，列举了20 个具有代表性的IA 型PI3K 抑制剂，并讨论了它们的分子抑制机制。

Reviews of class IA phosphatidylinositol-3 kinase’ effects on tumorigenesis as    well as the inhibitors’ molecular mechanism

LI Yue¹， MAO Wei-Feng²， ZHANG Yu-Bin^1*

(1 College of Life Science and Biotechnology， China Pharmaceutical University， Nanjing 211198， China; 2 WuXi AppTec (Shanghai) Co. Ltd， Shanghai 200131， China)

Abstract: Abstract: Phosphatidylinositol-3 kinase (PI3K) is an essential cellular signaling molecule which regulates many cellular functions including proliferation， differentiation， metabolism and apoptosis. Genes encoding PI3Ks are prone to mutation and amplification， leading to activation of PI3Ks， which correlates with tumorigenesis and development of various cancers. The pathway consisting of class IA PI3Ks and downstream signaling proteins participates in a set of events， such as cell proliferation， survival， adhesion and metastasis. In this article， we summarized the relationship between class IA PI3Ks (PI3Kα ， PI3Kβ and PI3Kδ) and tumorigenesis. In addition， 20 typical inhibitors against class IA PI3Ks in scientific research were listed and the molecular mechanism of inhibition was discussed.