The relationship between the bilayer to hexagonal phase transition temperature in membranes and protein kinase C activity.
A number of substances affect the activity of protein kinase C. Among uncharged and zwitterionic compounds, those which activate protein kinase C also lower the bilayer to hexagonal phase transition temperature of dielaidoylphosphatidylethanolamine while substances which inhibit protein kinase C raise this transition temperature. Using this criteria, we have identified 3 beta-chloro-5-cholestene, 5 beta-cholan-24-ol and eicosane as new protein kinase C activators and have shown that Z-Ser-Leu-NH2, Z-Gly-Leu-NH2, Z-Tyr-Leu-NH2, cyclosporin A and cholestan-3 beta, 5 alpha, 6 beta-triol are protein kinase C inhibitors.
Epand
R M
RM
Department of Biochemistry, McMaster University Health Sciences Centre, Hamilton, Ontario.
Stafford
A R
AR
Cheetham
J J
JJ
Bottega
R
R
Ball
E H
EH
D002784:Cholesterol / Q000494:pharmacology; D003524:Cyclosporins / Q000494:pharmacology; D004789:Enzyme Activation; D008051:Lipid Bilayers / Q000378:metabolism*; D010714:Phosphatidylethanolamines / Q000378:metabolism; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013696:Temperature; D013816:Thermodynamics
D003524:Cyclosporins; D008051:Lipid Bilayers; D010714:Phosphatidylethanolamines; D002784:Cholesterol; D011493:Protein Kinase C