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Article

Computational Study on the Effect of Inactivating/Activating Mutations on the Inhibition of MEK1 by Trametinib.

International journal of molecular sciences - 21 Mar 2020

Zhu Jingxuan, Li Congcong, Yang Hengzheng, Guo Xiaoqing, Huang Tianci, Han Weiwei

Abstract excerpt

Activation of the mitogen-activated protein kinase (MAPK) signaling pathway regulated by human MAP kinase 1 (MEK1) is associated with the carcinogenesis and progression of numerous cancers. In addition, two active mutations (P124S and E203K) have been reported to enhance the activity of MEK1, thereby eventually leading to the tumorigenesis of cancer. Trametinib is an MEK1 inhibitor for treating EML4-ALK-positive,...

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PMID: 32245216
DOI: 10.3390/ijms21062167
PMCID: PMC7139317

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