PI3K Inhibitors for Cancer Therapy: What has been Achieved So Far?

被引：38
作者：
Wu, Peng [1 ]
Liu, Tao [1 ]
Hu, Yongzhou [1 ]
机构：
[1] Zhejiang Univ, Coll Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Hangzhou 310058, Peoples R China
来源：
CURRENT MEDICINAL CHEMISTRY | 2009年 / 16卷 / 08期
关键词：
PI3K inhibitor; PI3K alpha; anticancer; structure-activity relationship (SAR); clinical trial; PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR; PHOSPHOINOSITIDE; 3-KINASE; BIOLOGICAL EVALUATION; PIK3CA GENE; 3-KINASE/MAMMALIAN TARGET; RAPAMYCIN INHIBITOR; FUNCTIONAL-ANALYSIS; NEGATIVE REGULATION; REGULATORY SUBUNIT; RESPIRATORY BURST;
D O I：
10.2174/092986709787581905
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
PI3K is a large duel lipid and protein kinase that catalyzes phosphorylation of the 3-hydroxyl position of phosphatidylinositides (PIs) and plays a crucial role in the cellular signaling network. Inhibition of the phosphatidylinositol 3-kinase (PI3K) signaling pathway is a newly identified strategy for the discovery and development of certain therapeutic agents. Among the various subtypes of PI3K, class IA PI3K alpha has gained increasing attention as a promising drug target for the treatment of cancer due to its frequent mutations and amplifications in various human cancers. Here, we discuss the insights gained so far relevant to the development of PI3K inhibitors for the treatment of human cancers. Emphasis is on the structure-activity relationship of PI3K inhibitors which bear the most significant PI3K alpha inhibitory activities. We also highlight PI3K inhibitors that are currently under clinical trials for cancers.
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收藏
页码：916 / 930
页数：15
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