Phosphatidylinositol 3-kinase (PI3K) inhibitors as cancer therapeutics

被引:242
作者
Akinleye, Akintunde [1 ,2 ]
Avvaru, Parthu [1 ,2 ]
Furqan, Muhammad [1 ,2 ]
Song, Yongping [3 ]
Liu, Delong [1 ,2 ,3 ]
机构
[1] New York Med Coll, Dept Med, Div Hematol Oncol, Valhalla, NY 10595 USA
[2] Westchester Cty Med Ctr, Valhalla, NY 10595 USA
[3] Zhengzhou Univ, Henan Canc Hosp, Zhengzhou 450052, Peoples R China
关键词
CHRONIC LYMPHOCYTIC-LEUKEMIA; DUAL PI3K/MTOR INHIBITOR; HUMAN PHOSPHOINOSITIDE 3-KINASE; BENDAMUSTINE PLUS RITUXIMAB; B-CELL; 3-KINASE/MAMMALIAN TARGET; RAPAMYCIN INHIBITOR; GROWTH-FACTOR; MANTLE-CELL; KINASE INHIBITOR;
D O I
10.1186/1756-8722-6-88
中图分类号
R73 [肿瘤学];
学科分类号
100214 [肿瘤学];
摘要
Phosphatidylinositol 3-kinases (PI3Ks) are lipid kinases that regulate diverse cellular processes including proliferation, adhesion, survival, and motility. Dysregulated PI3K pathway signaling occurs in one-third of human tumors. Aberrantly activated PI3K signaling also confers sensitivity and resistance to conventional therapies. PI3K has been recognized as an attractive molecular target for novel anti-cancer molecules. In the last few years, several classes of potent and selective small molecule PI3K inhibitors have been developed, and at least fifteen compounds have progressed into clinical trials as new anticancer drugs. Among these, idelalisib has advanced to phase III trials in patients with advanced indolent non-Hodgkin's lymphoma and mantle cell lymphoma. In this review, we summarized the major molecules of PI3K signaling pathway, and discussed the preclinical models and clinical trials of potent small-molecule PI3K inhibitors.
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页数:17
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