Factors underlying sensitivity of cancers to small-molecule kinase inhibitors

被引：257

作者：

Jaenne, Pasi A. ^{[3
,4
]}

Gray, Nathanael ^{[3
,4
]}

Settleman, Jeff ^{[1
,2
]}

机构：

[1] Massachusetts Gen Hosp, Ctr Canc, Charlestown, MA USA

[2] Harvard Univ, Sch Med, Charlestown, MA USA

[3] Dana Farber Canc Inst, Boston, MA 02115 USA

[4] Harvard Univ, Sch Med, Boston, MA USA

来源：

NATURE REVIEWS DRUG DISCOVERY | 2009年 / 8卷 / 09期

关键词：

CELL LUNG-CANCER; PHASE-II TRIAL; EML4-ALK FUSION GENE; TYROSINE KINASE; ACQUIRED-RESISTANCE; MAMMALIAN TARGET; BCR-ABL; ACTIVATING MUTATIONS; ANTITUMOR-ACTIVITY; ALK KINASE;

D O I：

10.1038/nrd2871

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Selective small-molecule kinase inhibitors have emerged over the past decade as an important class of anti-cancer agents, and have demonstrated impressive clinical efficacy in several different diseases, including relatively common malignancies such as breast and lung cancer. However, clinical benefit is typically limited to a fraction of treated patients. Genomic features of individual tumours contribute significantly to such clinical responses, and these seem to vary tremendously across patients. Additional factors, including pharmacogenomics, the tumour microenvironment and rapidly acquired drug resistance, also contribute to the clinical sensitivity of various cancers, and should be considered and applied in the development and use of new kinase inhibitors.

引用

页码：709 / 723

页数：15

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