Elongation factor-2 kinase: effective inhibition by the novel protein kinase inhibitor rottlerin and relative insensitivity towards staurosporine.
The elongation factor-2 (eEF-2) is selectively phosphorylated by the eEF-2 kinase (calmodulin-dependent kinase III). This phosphorylation can be inhibited by calmodulin antagonists, such as CGS 9343B (IC50 = 4 microM). The novel protein kinase inhibitor rottlerin is shown to suppress eEF-2 phosphorylation with an IC50 of 5.3 microM. By contrast, the eEF-2 kinase is rather resistant towards the potent but non-selective protein kinase inhibitor staurosporine (IC50 > 50 microM) and thus can be differentiated from most other protein kinases that are suppressed by staurosporine in the nM range.
Gschwendt
M
M
German Cancer Research Center, Heidelberg.
Kittstein
W
W
Marks
F
F
D000098:Acetophenones / Q000494:pharmacology*; D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D001578:Benzopyrans / Q000494:pharmacology*; D017871:Calcium-Calmodulin-Dependent Protein Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051379:Mice; D010766:Phosphorylation; D047428:Protein Kinase Inhibitors; D019311:Staurosporine
D000098:Acetophenones; D000470:Alkaloids; D001578:Benzopyrans; D047428:Protein Kinase Inhibitors; C085746:rottlerin; D017871:Calcium-Calmodulin-Dependent Protein Kinases; D019311:Staurosporine