Zwitterionic amphiphiles that raise the bilayer to hexagonal phase transition temperature inhibit protein kinase C The exception that proves the rule

FEBS Letters

Wang, Jian¹  Epand, Raquel F.¹  Stafford, Alan¹  Epand, Richard M.¹ 

[1]Department of Biochemistry, McMaster University, Health Sciences Centre, 1200 Main Street West, Hamilton, Ont. L8N 3Z5, Canada

关键词: Protein kinase C;    Hexagonal phase;    amphiphile;    Protein kinase C;    PKC;    Th;    bilayer to hexagonal phase transition temperature;    CPP;    cholesterylphosphorylethylpyridinium;    ODPP;    octadecylphosphorylethylpyridinium;    CPMP;    cholesterylphosphorylethyl-N-methyl piperidinium;    ODPC;    octadecylphosphorylcholine;    PS;    phosphatidylserine;   

DOI  :  10.1016/0014-5793(92)80629-U

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

We synthesized the zwitterionic amphiphile cholesterylphosphorylethylpyridinium. This substance activated protein kinase C (PKC) in a micelle-based assay, but in a vesicle assay it was inhibitory. An analog of this compound, in which the pyridine ring is saturated and the nitrogen methylated, showed similar behaviour with PKC. Replacing cholesterol by an aliphatic alcohol lowered the extent of activation in the micelle assay. These results demonstrate that, with some membrane additives, the vesicle and micelle assays give opposite results. Results from the membrane-based vesicle assay for PKC are in accord with the generalization that zwitterionic amphiphiles that raise the bilayer to hexagonal phase transition temperature in model membranes are inhibitors of PKC

【 授权许可】

Unknown