Alkyl analogs of diacylglycerol as activators of protein kinase C

FEBS Letters

Heymans, Françoise¹  Marrec, Noël¹  Da Silva, Corinne¹  Godfroid, Jean-Jacques¹  Castagna, Monique¹ 

[1] Laboratoire de Pharmacochimie Moléculaire, Université Paris VII, 2 Place Jussieu, 75251 Paris Cedex 05, and IRSC, 7, rue Guy Moquet, 94802 Villejuif Cedex, France

关键词: Protein kinase C;    Diacylglycerol;    Alkyl analog;    diC10;    1;    2-O-didecanoyl-rac-glycerol;    AAG-16;    1-O-hexadecyl-2-O-acetylglycerol;    AAG-18;    1-O-octadecyl-2-O-acetylglycerol;    TPA;    12-O-tetra-decanoylphorbol 13-acetate;    DMF;    dimethylformamide;    TMS;    tetramethylsilane;   

DOI  :  10.1016/0014-5793(87)81013-X

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Diacylglycerols which activate protein kinase C have the 1,2-sn configuration. Short-chain saturated fatty acids or long-chain unsaturated fatty acids are required for supporting the potency of these lipids. Using alkyl analogs such as 1-O-decyl-2-O-decanoylglycerol, 1-O-decanoyl-2-O-decylglycerol, 1,2-O-didecyl-glycerol, 1-O-hexadecyl-2-O-acetylglycerol and 1-O-decyl-2-O-acetylglycerol, we showed that the ether bond was consistently associated with a loss of activity to varying extents. The results suggest that the ester bond in the 1-position is a major determinant of diacylglycerol-mediated protein kinase activation.

【 授权许可】

Unknown