摘要
丝裂原活化蛋白激酶(MAPK)通路是肿瘤发生过程中众多细胞过程的关键因素之一,提示其为妇科肿瘤的潜在治疗靶点。MAPKs连接基因表达途径和外部刺激。它们包括一个由Ras, Raf或MAP3K, MEK或MAP2K, ERK或MAPK组成的网络。其中,MEK连接上游激活因子和下游相应的激活因子,是新型癌症治疗中极具吸引力的分子靶点。MEK抑制剂是首批进入临床试验的MAPK通路抑制剂之一。最近开发了几种药物作为MEK抑制剂。在过去的十年中,MEK1/2抑制剂在治疗这种恶性肿瘤方面表现出了良好的疗效和抗癌活性,引起了广泛关注。本文中,我们总结了MAPK/MEK/ERK通路在妇科癌症发病机制中的作用,特别强调了临床环境中的MEK抑制剂,包括PD-0325901、Selumetinib、Cobimetinib、Refametinib、Trametinib、Pimasertib、MEK162和WX-554在妇科癌症中的作用。
关键词: 丝裂原活化蛋白激酶(MAPK),MEK1/2抑制剂,妇科癌症,致瘤,抗癌活性,WX-554。
Current Cancer Drug Targets
Title:The Therapeutic Potential of MEK1/2 Inhibitors in the Treatment of Gynecological Cancers: Rational Strategies and Recent Progress
Volume: 20 Issue: 6
关键词: 丝裂原活化蛋白激酶(MAPK),MEK1/2抑制剂,妇科癌症,致瘤,抗癌活性,WX-554。
摘要: The mitogen-activated protein kinase (MAPK) pathway is among the key factors in numerous cellular processes involved in tumorigenesis, suggesting it as a potential therapeutic target in gynecological cancer. MAPKs connect gene expression pathways and external stimulations. They include a network consisting of Ras, Raf or MAP3K, MEK or MAP2K, ERK or MAPK. Among these, MEK is an attractive molecular target of novel cancer therapeutics as it joints upstream activators and their corresponding downstream targets. MEK inhibitors were among the first inhibitors of the MAPK pathway entering into clinical trials. Several drugs have recently been developed as MEK inhibitors. MEK1/2 inhibitors demonstrate promising efficacy and anticancer activity to treat this malignancy and captured much attention in the past decade. Here, we summarize the role of MAPK/MEK/ERK pathway in the pathogenesis of gynecological cancer, with particular emphasis on MEK inhibitors in clinical settings, including PD-0325901, Selumetinib, Cobimetinib, Refametinib, Trametinib, Pimasertib, MEK162 and WX-554 in gynecologic cancers.
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Cite this article as:
The Therapeutic Potential of MEK1/2 Inhibitors in the Treatment of Gynecological Cancers: Rational Strategies and Recent Progress, Current Cancer Drug Targets 2020; 20 (6) . https://dx.doi.org/10.2174/1568009620666200424144303
DOI https://dx.doi.org/10.2174/1568009620666200424144303 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
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