摘要
RAS-RAF-MEK-ERK信号通路(MAPK信号通路)在30%以上的人类癌症中高度激活。这一途径的异常激活主要是由于RAS或RAF基因的功能获得突变。此外,丝裂原激活蛋白激酶(MEK)在肿瘤发生、细胞增殖和凋亡抑制中的关键作用,使MEK抑制剂(MEKi)成为MAPK通路相关肿瘤靶向治疗的有吸引力的候选药物。几个高度选择性和有效的非ATP竞争的变构MEKi已经被开发出来,并导致了临床结果的实质性改善。然而,由于复杂通路的串扰和较差的药物溶解度,药物的疗效和反应率受到限制。纳米修饰在过去的几十年里为提高药物的疗效做出了巨大的贡献。本综述主要阐述MEK激酶在MAPK通路中的重要生物学地位,以突出MEKi的不可替代地位和临床地位。此外,还简要综述了增强药物疗效的纳米修复策略,以及纳米技术在MEKi相关的肿瘤治疗领域中的应用进展。最后,指出了阻碍纳米MEKi发展的障碍,并展望了纳米MEKi的发展前景。这篇内容丰富的报告为MEKi的临床发展奠定了基础,并概述了个性化癌症治疗的一种合理的前线治疗方法。
关键词: 纳米医药,修复策略,MAPK信号通路,MEK抑制剂,增强药物疗效,癌症的靶向诊疗。
图形摘要
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