Brody School of Medicine at East Carolina University, Department of Microbiology & Immunology, 600 Moye Boulevard, Greenville, NC 27858, USA.
Expert Opin Emerg Drugs. 2010 Jun;15(2):203-23. doi: 10.1517/14728210903282760.
The Ras/Raf/MEK/ERK pathway is often activated by genetic alterations in upstream signaling molecules. Integral components of this pathway such as Ras and B-Raf are also activated by mutation. The Ras/Raf/MEK/ERK pathway has profound effects on proliferative, apoptotic and differentiation pathways. This pathway can often be effectively silenced by MEK inhibitors. AREAS COVERED BY THIS REVIEW: This review will discuss targeting of MEK which could lead to novel methods to control abnormal proliferation which arises in cancer and other proliferative diseases. This review will cover the scientific literature from 1980 to present and is a follow on from a review which focused on Emerging Raf Inhibitors published in this same review series.
By reading this review the reader will understand the important roles that genetics play in the response of patients to MEK inhibitors, the potential of combining MEK inhibitors with other types of therapy, the prevention of cellular aging and the development of cancer stem cells.
Targeting MEK has been shown to be effective in suppressing many important pathways involved in cell growth and the prevention of apoptosis. MEK inhibitors have many potential therapeutic uses in the suppression of cancer, proliferative diseases and aging.
Ras/Raf/MEK/ERK 通路通常通过上游信号分子的遗传改变而被激活。该通路的基本组成部分，如 Ras 和 B-Raf，也会因突变而被激活。Ras/Raf/MEK/ERK 通路对增殖、凋亡和分化途径有深远的影响。MEK 抑制剂通常可以有效地沉默这条通路。
本篇综述将讨论 MEK 的靶向作用，这可能会导致控制癌症和其他增殖性疾病中异常增殖的新方法。本篇综述将涵盖从 1980 年至今的科学文献，是该综述系列中一篇关于新兴 Raf 抑制剂的综述的后续内容。
通过阅读这篇综述，读者将了解遗传学在患者对 MEK 抑制剂反应中的重要作用、将 MEK 抑制剂与其他类型的治疗相结合的潜力、预防细胞衰老和癌症干细胞的发展。
已经证明靶向 MEK 可以有效地抑制细胞生长和防止细胞凋亡的许多重要途径。MEK 抑制剂在抑制癌症、增殖性疾病和衰老方面有许多潜在的治疗用途。
