MEK inhibitor - Wikipedia
网页A MEK inhibitor is a chemical or drug that inhibits the mitogen-activated protein kinase kinase enzymes MEK1 and/or MEK2. They can be used to affect the MAPK/ERK pathway which is often overactive in some cancers.
MEK inhibitors for the treatment of non-small cell lung cancer
网页2021年1月5日 · According to the reported findings, the combination of MEK inhibitors with chemotherapy, immune checkpoint inhibitors, epidermal growth factor receptor-tyrosine kinase inhibitors or BRAF inhibitors is highly significant for improving clinical efficacy and causing delay in the occurrence of drug resistance.
MEK 抑制剂 - 知乎 - 知乎专栏
网页2021年10月27日 · 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 ...
MEK Inhibitor Mechanism of Action, Side Effects, and Uses
网页2019年8月21日 · MEK inhibitors bind to and inhibit MEK, inhibiting MEK-dependent cell signaling. This inhibition leads to cell death and the inhibition of tumor growth. These are...
MEK inhibitors in cancer treatment: structural insights, regulation ...
网页2023年8月10日 · To date, 4 MEK inhibitors i.e., trametinib, cobimetinib, selumetinib, and binimetinib have been approved by the FDA and several are under clinical trials. In this review, we have highlighted structural insights into the MEK1/2 proteins, such as the αC-helix, catalytic loop, P-loop, F-helix, hydrophobic pocket, and DFG motif.
MEK1 and MEK2 inhibitors and cancer therapy: the long and
网页2015年9月24日 · New drugs that inhibit RAF or MEK1 and MEK2 have recently been approved or are currently undergoing late-stage clinical evaluation. In this Review, we consider the ERK pathway, focusing...
Current Development Status of MEK Inhibitors - PMC
网页2017年9月26日 · In recent years, MEK inhibitors have been discovered and developed very rapidly. Trametinib became the first approved drug among MEK inhibitors, and cobimetinib soon followed suit. MEK inhibitors as single agents or in combination with other therapies have shown to be efficacious in treating melanoma, lung cancer, and …
The biology and clinical development of MEK inhibitors for …
网页The role of MEK in cancer and the mechanism of action of MEK inhibitors is reviewed. Furthermore, MEK inhibitors that are available in standard practice, as well as those most advanced in clinical development, are discussed.
Structural basis for the action of the drug trametinib at KSR-bound MEK
网页2020年9月14日 · Crystal structures of the MEK kinase bound to the scaffold protein KSR and various MEK inhibitors, including the anti-cancer drug trametinib, reveal the molecular and functional mechanisms...
MEK in cancer and cancer therapy - PubMed
网页MEK inhibitors (MEKi) are currently under evaluation in clinical trials and many have shown activity. In this review, we comprehensively examine the role of the MEK pathway in carcinogenesis and its therapeutic potential in cancer patients, with a focus on MEKi.
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