TABLE 2.

The inhibitors/activators targeting eEF2K.

Name of compound	Structure	Principle	Type of pathologies	References
A484954 (7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido [2,3-days] pyrimidine-6-carboxamide)		ATP competitive inhibitor, but CaM-independent Demonstrates almost no cytotoxicity	Hypertension	Kodama et al. (2018); Xie et al. (2018); Kodama et al. (2019)
			Atherosclerosis
			Breast cancer
			Lung cancer
			TNBC
Rottlerin (5,7-dihydroxy-2,2-dimethyl-6-(2,4,6-trihydroxy-3-methyl-5-acetylbenzyl)-8-cinnamoyl-1,2-chromine)		Natural product, PKC δ (protein kinase Cδ) inhibitor	Glioma	Gschwendt et al. (1994)
Compound 34 (Thieno [2–3-b]pyridine analogues)		ATP competitive inhibitor	Colorectal cancer	Lockman et al. (2010)
NH125 (1-benzyl-3-cetyl-2-methylimidazolium iodide)		Histidine protein kinase inhibitor, selective inhibitor of eEF2K in vitro	Glioma	Arora et al. (2003); Arora et al. (2004); Lockman et al. (2010); Zhang et al. (2011); Zhu et al. (2017); Xie et al. (2018)
			Esophageal squamous cell carcinoma
			Breast cancer
			Lung cancer
Geldanamycin (GA)		Natural product, blockage of eEF2K and Hsp90	Human glioma	Yang et al. (2001)
17-AAG (17-allylamino-17-demethoxygeldanamycin)		Less toxic and less potent derivative of GA, inhibitor of Hsp/protein interactions	Human glioma	Yang et al. (2001)
Cefatrizine		Induces ER stress	Breast cancer	Yao et al. (2016)
Nelfinavir (NFR)		HIV aspartyl protease inhibition, also triggers eEF2K activation	-	De Gassart et al. (2016)
JAN-384, -452, -613, -849	Unknown	Unknown	Breast cancer	Kenney et al. (2016); Moore et al. (2016); Xie et al. (2018)
			Lung cancer
TS-2 (4-ethyl-4-hydroxy-2-p-tolyl-5,6-dihydro-4H-1,3-selenazine)		Multiple tyrosine kinase inhibitors, including protein kinase A (PKA), protein kinase C (PKC), and protein tyrosine kinase (PTK)	None	Cho et al. (2000); Lockman et al. (2010)
TS-4 (4-hydroxy-6-isopropyl-4-methyl-2-p-tolyl-5,6-dihydro-4H-1,3-selenazine)		Multiple tyrosine kinase inhibitors, including PKA, PKC, and PTK	None	Cho et al. (2000); Lockman et al. (2010)
TX-1918 (2-hydroxyarylidene-4-cyclopentene-1,3-dione)		Protein tyrosine kinase inhibitor	TNBC	Hori et al. (2002); Ju et al. (2021)
Compound A1		Derived from the core structure of rottlerin; however, the detailed mechanism is unknown	TNBC	Comert Onder et al. (2020)
Compound A2		Derived from the core structure of rottlerin; however, the detailed mechanism is unknown	TNBC	Comert Onder et al. (2020)
Thymoquinone (TQ)		Induction of tumor suppressor, miR-603 and NF-kB inhibition	TNBC	Kabil et al. (2018)
21L (2.4-dichloro)		ATP-competitive inhibitor, could stably bind to the ATP binding site of eEF2K	Breast cancer (in vivo and in vitro)	Guo et al. (2018)
		Induces apoptosis pathway