Targeting cancer with small molecule kinase inhibitors

被引：2073

作者：

Zhang, Jianming ^{[1
]}

Yang, Priscilla L. ^{[2
]}

Gray, Nathanael S. ^{[1
]}

机构：

[1] Harvard Univ, Sch Med, Dept Biol Chem & Mol Pharmacol, Dana Farber Canc Inst,Dept Canc Biol, Boston, MA 02115 USA

[2] Harvard Univ, Sch Med, Dept Microbiol & Mol Genet, Boston, MA 02115 USA

来源：

NATURE REVIEWS CANCER | 2009年 / 9卷 / 01期

关键词：

CHRONIC MYELOID-LEUKEMIA; CHRONIC MYELOGENOUS LEUKEMIA; RECEPTOR TYROSINE KINASE; ACTIVATED PROTEIN-KINASE; GROWTH-FACTOR RECEPTOR; RIBOSOMAL S6 KINASE; ABL KINASE; BCR-ABL; ANTITUMOR-ACTIVITY; CRYSTAL-STRUCTURE;

D O I：

10.1038/nrc2559

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Deregulation of kinase activity has emerged as a major mechanism by which cancer cells evade normal physiological constraints on growth and survival. To date, 11 kinase inhibitors have received US Food and Drug Administration approval as cancer treatments, and there are considerable efforts to develop selective small molecule inhibitors for a host of other kinases that are implicated in cancer and other diseases. Herein we discuss the current challenges in the field, such as designing selective inhibitors and developing strategies to overcome resistance mutations. This Review provides a broad overview of some of the approaches currently used to discover and characterize new kinase inhibitors.

引用

页码：28 / 39

页数：12

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