期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 64, 期 13, 页码 8870-8883出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.0c02218
关键词
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资金
- National Natural Science Foundation of China [81673455, 21772131, 31970374]
- Key R&D Program of Sichuan Province [2021YFS0046]
- National Science and Technology Major Project of the Ministry of Science and Technology of China [2018ZX09735005]
Eukaryotic elongation factor 2 kinase (eEF2K) is a key negative regulator of protein synthesis in tumorigenesis, with potential for cancer therapy improvement through single-target inhibitors, repurposed drugs, dual-target inhibitors, drug combination strategies, and emerging technologies.
Eukaryotic elongation factor 2 kinase (eEF2K), a member of the atypical protein kinase family of alpha-kinases, is well-known as a negative regulator of protein synthesis by phosphorylating eEF2. Notably, eEF2K functions as a key regulator of several cellular processes, leading to tumorigenesis. To date, some small-molecule compounds have been reported as potential eEF2K inhibitors in cancer drug discovery. However, an ideal targeted drug design still faces huge challenges. Alternatively, other design strategies, such as repurposed drugs, dual-target drugs, and drug combination strategies, provide insights into the improvement of cancer treatment. Here, we summarize the crucial eEF2K-modulating pathways in cancer, including AMPK, REDD1, and Src. Moreover, we discuss the inhibition of eEF2K with single-target inhibitors, repurposed drugs, dual-target inhibitors, drug combination strategies, and other emerging technologies for therapeutic purposes. Together, these inspiring findings provide insights into a promising strategy for inhibiting eEF2K with small-molecule compounds to improve potential cancer therapy.
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