Cholesterylphosphoryldimethylethanolamine is a zwitterionic compound which is a good bilayer stabilizer. As has been found with many other compounds having these properties, cholesterylphosphoryldimethylethanolamine is found to be a potent inhibitor of protein kinase C in both vesicle and micelle assay systems. The kinetics of the inhibition in Triton X-100 micelles was non-competitive with respect to ATP, histone, diolein, phorbol ester and Ca2+. It has a Ki of about 30 μm. The inhibition kinetics as a function of phosphatidylserine concentration is more complex but suggestive of competitive inhibition. Cholesterylphosphoryldimethylethanolamine does not prevent the partitioning of protein kinase C into the membrane. This inhibitor lowers the Ca2+-phosphatidylserine-independent phosphorylation of protamine sulfate by protein kinase C and directly affects the catalytic segment of the enzyme generated by tryptic hydrolysis. Thus, this zwitterionic bilayer stabilizing inhibitor of protein kinase C both competes with the binding of phosphatidylserine as well as affects the active site of protein kinase C.
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June 01 1989
Studies on the mechanism of action of a bilayer stabilizing inhibitor of protein kinase C: Cholesterylphosphoryldimethylethanolamine
Richard M. Epand;
Richard M. Epand
1Department of Biochemistry, McMaster University, Health Sciences Centre, 1200 Main Street West, Hamilton, Ontario, Canada, L8N 3Z5
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Alan R. Stafford;
Alan R. Stafford
1Department of Biochemistry, McMaster University, Health Sciences Centre, 1200 Main Street West, Hamilton, Ontario, Canada, L8N 3Z5
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Remo Bottega;
Remo Bottega
1Department of Biochemistry, McMaster University, Health Sciences Centre, 1200 Main Street West, Hamilton, Ontario, Canada, L8N 3Z5
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Eric H. Ball
Eric H. Ball
1Department of Biochemistry, University of Western Ontario, London, Ontario
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Publisher: Portland Press Ltd
Received:
October 16 1988
Online ISSN: 1573-4935
Print ISSN: 0144-8463
© 1989 Plenum Publishing Corporation
1989
Biosci Rep (1989) 9 (3): 315–328.
Article history
Received:
October 16 1988
Citation
Richard M. Epand, Alan R. Stafford, Remo Bottega, Eric H. Ball; Studies on the mechanism of action of a bilayer stabilizing inhibitor of protein kinase C: Cholesterylphosphoryldimethylethanolamine. Biosci Rep 1 June 1989; 9 (3): 315–328. doi: https://doi.org/10.1007/BF01114684
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