Clinical Experience with Aurora Kinase Inhibitors: A Review

被引：83

作者：

Boss, David S. ^{[1
]}

Beijnen, Jos H. ^{[1
,2
,3
]}

Schellens, Jan H. M. ^{[1
,2
]}

机构：

[1] Netherlands Canc Inst, Div Clin Pharmacol, Dept Med Oncol, NL-1066 CX Amsterdam, Netherlands

[2] Univ Utrecht, Fac Sci, Dept Pharmaceut Sci, Sect Biomed Anal,Div Drug Toxicol, Utrecht, Netherlands

[3] Slotervaart Hosp, Dept Pharm & Pharmacol, Amsterdam, Netherlands

来源：

ONCOLOGIST | 2009年 / 14卷 / 08期

关键词：

Aurora kinase; Mitosis; Targeted therapy; Drug development; Clinical trial; SMALL-MOLECULE INHIBITOR; CHROMOSOMAL PASSENGER COMPLEX; SPINDLE-ASSEMBLY CHECKPOINT; HISTONE H3 PHOSPHORYLATION; SUPPRESSES TUMOR-GROWTH; LEUKEMIA CELL-LINES; B-KINASE; A KINASE; MITOTIC PHOSPHORYLATION; DOWN-REGULATION;

D O I：

10.1634/theoncologist.2009-0019

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 [肿瘤学];

摘要：

The aurora kinase family of serine/threonine kinases comprises three members, designated auroras A, B, and C. Auroras A and B are essential components of the mitotic pathway, ensuring proper chromosome assembly, formation of the mitotic spindle, and cytokinesis. The role of aurora C is less clear. Overexpression of aurora A and B has been observed in several tumor types, and has been linked with a poor prognosis of cancer patients. Several small molecules targeting aurora kinases A and B or both have been evaluated preclinically and in early phase I trials. In this review we aim to summarize the most recent advances in the development of aurora kinase inhibitors, with a focus on the clinical data. The Oncologist 2009; 14: 780-793

引用

页码：780 / 793

页数：14

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