The genesis of Zelboraf: Targeting mutant B-Raf in melanoma

被引：8

作者：

Davis, Matthew J. ^{[1
]}

Schlessinger, Joseph ^{[1
]}

机构：

[1] Yale Univ, Sch Med, Dept Pharmacol, New Haven, CT 06520 USA

来源：

JOURNAL OF CELL BIOLOGY | 2012年 / 199卷 / 01期

关键词：

BRAF MUTATION; V-RAF; KINASE; RESISTANCE; INHIBITOR; SURVIVAL; FAMILY; MEK;

D O I：

10.1083/jcb.201205167

中图分类号：

Q2 [细胞生物学];

学科分类号：

071013 [干细胞生物学];

摘要：

The protein kinase B-Raf is a critical component of the Ras/MAPK signaling pathway. An oncogenic B-Raf mutation that constitutively activates the kinase was identified in similar to 50% of melanoma patients and in other cancers. A structure-guided drug discovery approach enabled the development of Zelboraf, a targeted inhibitor of oncogenic B-Raf. This drug has been used successfully in the clinic to treat metastatic melanoma patients harboring B-Raf mutations.

引用

页码：15 / 19

页数：5

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