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新型B-Raf激酶抑制剂研究进展

Adwances in the research of newly B-Raf kinase inhibitors
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摘要 Ras-Raf-Mek-Erk信号转导通路在调控细胞生长,分化和增殖起着至关重要的作用。而Ras或者B-Raf的突变都会导致肿瘤的发生。B-Raf被激活后的体细胞突变率在黑色素瘤中高达50%~70%,卵巢癌中达35%,甲状腺癌中达30%,结肠癌中达10%,因此B-RafV600E作为治疗人类癌症的靶标而日益受到研究者的关注。本综述主要从结构优化对活性的影响上阐述了近两年来新型B-Raf激酶抑制剂的最新研究进展。 The Ras-Raf-MEK-ERK signal transduction pathway（ERK pathway） plays a key role in cellular growth,division and proliferation.Mutations of either Ras or B-Raf lead to the development of human cancers.Activating B-Raf mutations have been found in melanomas（50~70%）,ovarian cancer（35%）,papillary thyroid cancers（30%） and colorectal cancer（10%）.Therefore,B-RafV600E is a high-interest therapeutic target for the treatment of human cancers.This review put emphasis on B-Raf kinase inhibitors which was newly approved in rencent literatures,including the effect of B-Raf kinase′s activity brought by structural modification.
作者 颜彩虹 唐伟方 陈亚东 刘海春 陆涛
机构地区 中国药科大学有机教研室
出处 《海峡药学》 2011年第6期1-4,共4页 Strait Pharmaceutical Journal
关键词 Raf激酶 激酶抑制剂 B-RafV600E 肿瘤治疗 Raf kinase Kinase inhibitor B-RafV600E Tumor therapy
分类号 R318 [医药卫生—生物医学工程]
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参考文献22

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二级参考文献34

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海峡药学
2011年 第6期

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