Inhibition of protein kinase CKII activity by resveratrol, a natural compound in red wine and grapes.
Resveratrol is a phytoalexin found in grapes and other foods that has been shown to have anticancer and anti-inflammatory effects. Because protein kinase CKII is involved in cell proliferation and oncogenesis, we examined whether resveratrol could modulate CKII activity. Resveratrol was shown to inhibit the phosphotransferase activity of CKII with IC(50) of about 10 microM. Steady state studies revealed that resveratrol acted as a competitive inhibitor with respect to the substrate ATP. A value of 1.2 microM was obtained for the apparent K(i). Resveratrol also inhibited the catalytic reaction of CKII with GTP as substrate. Furthermore, resveratrol inhibits endogenous CKII activity on protein substrates in HeLa cell lysates. These results suggest that resveratrol is likely to function by inhibiting oncogenic disease, at least in part, through the inhibition of CKII activity.
Department of Biochemistry, College of Natural Sciences, Kyungpook National University, Taegu 702-701, South Korea.
Soo-Hyun
SH
Yoon
Yun-Sook
YS
Kim
Sa-Youl
SY
Ghim
Bang-Ho
BH
Song
Young-Seuk
YS
Bae
D000255:Adenosine Triphosphate / Q000378:metabolism; D016588:Anticarcinogenic Agents / Q000494:pharmacology*; D047390:Casein Kinase II; D002384:Catalysis; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D010766:Phosphorylation; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D000077185:Resveratrol; D013267:Stilbenes / Q000494:pharmacology*; D027843:Vitis / Q000737:chemistry*; D014920:Wine / Q000032:analysis*
D016588:Anticarcinogenic Agents; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D013267:Stilbenes; D000255:Adenosine Triphosphate; D047390:Casein Kinase II; D017346:Protein Serine-Threonine Kinases; D000077185:Resveratrol