Targeting the RAS pathway by mitogen-activated protein kinase inhibitors

被引：12

作者：

Kiessling, Michael K. ^{[1
]}

Rogler, Gerhard ^{[1
]}

机构：

[1] Univ Zurich Hosp, Dept Gastroenterol & Hepatol, Raemistr 100, CH-8091 Zurich, Switzerland

来源：

SWISS MEDICAL WEEKLY | 2015年 / 145卷

关键词：

NRAS mutations; HRAS mutations; MEK inhibitor; ORAL MEK INHIBITOR; SMALL-CELL LUNG; BRAF-MUTANT MELANOMA; PHASE-II; OPEN-LABEL; AZD6244; ARRY-142886; METASTATIC MELANOMA; COMBINATION THERAPY; TUMOR PROGRESSION; DOSE-ESCALATION;

D O I：

10.4414/smw.2015.14207

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

Targeting of oncogenic driver mutations with small-molecule inhibitors resulted in powerful treatment options for cancer patients in recent years. The RAS (rat sarcoma) pathway is among the most frequently mutated pathways in human cancer. Whereas targeting mutant Kirsten RAS (KRAS) remains difficult, mutant B rapidly accelerated fibrosarcoma (BRAF) kinase is an established drug target in cancer. Now data show that neuroblastoma RAS (NRAS) and even Harvey RAS (HRAS) mutations could be predictive markers for treatment with mitogen-activated protein kinase (MEK) inhibitors. This review discusses recent preclinical and clinical studies of MEK inhibitors in BRAF and RAS mutant cancer.

引用

页数：9

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