The CDK inhibitors in cancer research and therapy

被引：193

作者：

Cicenas, Jonas ^{[1
,2
]}

Valius, Mindaugas ^{[3
]}

机构：

[1] Univ Fribourg, Inst Anat, Dept Med, CH-1700 Fribourg, Switzerland

[2] MAP Kinase Resource, Bern, Switzerland

[3] Lithuania Acad Sci, Inst Biochem, Dept Dev Biol, LT-232600 Vilnius, Lithuania

来源：

JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY | 2011年 / 137卷 / 10期

关键词：

CDK; Kinases; Small-molecule inhibitors; Cancer; Cell cycle; DEPENDENT KINASE INHIBITOR; ADVANCED SOLID TUMORS; CELL LUNG-CANCER; PHASE-II TRIAL; CHRONIC LYMPHOCYTIC-LEUKEMIA; GROWTH-FACTOR RECEPTOR; ACTIVITY IN-VIVO; BREAST-CANCER; CARCINOMA-CELLS; POOR-PROGNOSIS;

D O I：

10.1007/s00432-011-1039-4

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Chemical compounds that interfere with an enzymatic function of kinases are useful for gaining insight into the complicated biochemical processes in mammalian cells. Cyclin-dependent kinases (CDK) play an essential role in the control of the cell cycle and/or proliferation. These kinases as well as their regulators are frequently deregulated in diVerent human tumors. Aberrations in CDK activity have also been observed in viral infections, Alzheimer's, Parkinson's diseases, ischemia and some proliferative disorders. This led to an intensive search for small-molecule CDK inhibitors not only for research purposes, but also for therapeutic applications. Here, we discuss seventeen CDK inhibitors and their use in cancer research or therapy. This review should help researchers to decide which inhibitor is best suited for the specific purpose of their research. For this purpose, the targets, commercial availability and IC50 values are provided for each inhibitor. The review will also provide an overview of the clinical studies performed with some of these inhibitors.

引用

页码：1409 / 1418

页数：10

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