Interaction of berbamine compound E6 and calmodulin-dependent myosin light chain kinase.
The interaction of the berbamine compound E6 and calmodulin (CaM)-dependent myosin light chain kinase (MLCK) has been studied. The experimental results showed that the inhibition of MLCK activity was increased with increasing amounts of E6 and was overcome completely by the addition of excessive CaM. The stimulatory activity of MLCK induced by CaM was gradually inhibited by the increasing concentrations of compound E6, showing that the inhibition of MLCK activity by compound E6 was concentration dependent; and the Ki was 0.95 microM. Compound E6 diminished the fluorescence intensity of dansyl-labeled CaM and the intensity was increased gradually by the addition of different amounts of CaM. Compound E6 had no effect on the activity of MLCK fragments produced by limited trypsinization, and it is a novel and considerably potent calmodulin antagonist.
Hu
Z Y
ZY
Division of Biochemistry, China Pharmaceutical University, Nanjing, Jiangsu.
Gong
Y S
YS
Huang
W L
WL
D000470:Alkaloids / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D044182:Benzylisoquinolines; D002147:Calmodulin / Q000378:metabolism* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D007700:Kinetics; D009219:Myosin-Light-Chain Kinase / Q000037:antagonists & inhibitors / Q000378:metabolism*; D014357:Trypsin
D000470:Alkaloids; D044182:Benzylisoquinolines; D002147:Calmodulin; D009219:Myosin-Light-Chain Kinase; D014357:Trypsin; C027870:berbamine