丝裂原活化的细胞外信号调节激酶(mitogen-activated extracellular signal-regulated kinase,MEK)是一种可磷酸化靶蛋白上丝氨酸/苏氨酸和酪氨酸残基的双特异性激酶,也是RASRAF-MEK-ERK信号转导通路的主要组分。
MEK信号通路参与了细胞凋亡,细胞周期进行,细胞迁移、分化、代谢和细胞增殖等众多过程的调节。大量研究表明,MEK结构及其表达水平的改变与肿瘤等多种疾病的发生密切相关。
PMEK抑制剂的临床研究现状及激酶活性
参考文献
[1]MEK inhibitors for the treatment of non-small cell lung cancer. Journal of Hematology & Oncology volume 14, Article number: 1 (2021)
[2] Synergistic inhibition of MEK and reciprocal feedback networks for targeted intervention in malignancy Cancer Biol Med. 2019 Aug; 16(3): 415–434.
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