Ten things you should know about protein kinases: IUPHAR Review 14

被引：260

作者：

Fabbro, Doriano ^{[1
]}

Cowan-Jacob, Sandra W. ^{[2
]}

Moebitz, Henrik ^{[2
]}

机构：

[1] PIQUR Therapeut, CH-4057 Basel, Switzerland

[2] Novartis Inst Biomed Res, Basel, Switzerland

来源：

BRITISH JOURNAL OF PHARMACOLOGY | 2015年 / 172卷 / 11期

基金：

英国惠康基金;

关键词：

CHRONIC MYELOID-LEUKEMIA; CELL LUNG-CANCER; TYROSINE KINASE; SMALL-MOLECULE; BCR-ABL; ACQUIRED-RESISTANCE; SELECTIVE INHIBITOR; IRREVERSIBLE INHIBITORS; TARGETING KINASES; MAP KINASE;

D O I：

10.1111/bph.13096

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Many human malignancies are associated with aberrant regulation of protein or lipid kinases due to mutations, chromosomal rearrangements and/or gene amplification. Protein and lipid kinases represent an important target class for treating human disorders. This review focus on the 10 things you should know about protein kinases and their inhibitors', including a short introduction on the history of protein kinases and their inhibitors and ending with a perspective on kinase drug discovery. Although the 10 things' have been, to a certain extent, chosen arbitrarily, they cover in a comprehensive way the past and present efforts in kinase drug discovery and summarize the status quo of the current kinase inhibitors as well as knowledge about kinase structure and binding modes. Besides describing the potentials of protein kinase inhibitors as drugs, this review also focus on their limitations, particularly on how to circumvent emerging resistance against kinase inhibitors in oncological indications.

引用

页码：2675 / 2700

页数：26

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