Therapeutic targets in melanoma: map kinase pathway.

Therapeutic targets in melanoma: map kinase pathway.
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DOI:
10.1007/s11912-006-0065-x
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发表时间:
2006-09-01
影响因子:
4.7
通讯作者:
Ibrahim, Nageatte
Ibrahim, Nageatte
中科院分区:
医学2区
文献类型:
--
作者:
Haluska, Frank G;Ibrahim, Nageatte

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在我们对黑色素瘤发病机制中发生的基因改变的理解上的最新进展为治疗提供了令人兴奋的机会。黑色素瘤最重要的信号通路位于NRAS下游:RAS-BRAF-MAPK通路。由于BRAF本身是一种很有吸引力的药物底物,而且BRAF功能在黑色素瘤的发生发展中起着重要的作用,BRAF癌基因的高突变率已引起了人们的极大关注,突变率接近60%。针对BRAF的药物,如索拉非尼,以及具有BRAF上游和下游功能的新分子,正在积极研究中。
Recent progress in our understanding of the genetic alterations that occur in the pathogenesis of melanoma provides exciting opportunities for therapy. The most important signaling pathways in melanoma lie downstream of NRAS: the RAS-BRAF-MAPK pathway. A great deal of attention has been focused on the high mutation rate in the BRAF oncogene, which approaches 60%, because BRAF itself is an appealing drug substrate and because of the central contribution of BRAF function to melanoma development that the mutation rate signifies. Agents that specifically target BRAF, such as sorafenib, as well as new molecules that function both upstream and downstream of BRAF, are being actively investigated.