CCK2 (CCKB/gastrin) receptor mediates rapid protein kinase D (PKD) activation through a protein kinase C‐dependent pathway

FEBS Letters

Chiu, Terence¹  Rozengurt, Enrique¹ 

[1] Department of Medicine, UCLA School of Medicine and Molecular Biology Institute, 900 Veteran Avenue, Warren Hall, Room 11-124, University of California, Los Angeles, CA 90095-1786, USA

关键词: Gastrin;    Cholecystokinin;    Rat-1 cell;    Protein kinase C;    Protein kinase D;    AEBSF;    4-(2-aminoethyl)-benzenesulfonyl fluoride hydrochloride;    CCK-8;    sulfated cholecystokinin octapeptide;    DAG;    diacylglycerol;    DMEM;    Dulbecco's modified Eagle's medium;    G proteins;    guanine nucleotide-binding regulatory proteins;    GF-I;    bisindolylmaleimide I (GF 109203X);    GPCR;    G protein-coupled receptor;    PAGE;    polyacrylamide gel electrophoresis;    PBS;    phosphate-buffered saline;    PKC;    protein kinase C;    PKD;    protein kinase D;   

DOI  :  10.1016/S0014-5793(01)02076-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Addition of gastrin or cholecystokinin octapeptide (CCK-8) to cultures of Rat-1 cells stably transfected with the CCK2 (CCK_B/gastrin) receptor induced protein kinase D (PKD) activation that was detectable within 1 min and reached a maximum (∼10-fold) after 2.5 min of hormonal stimulation. Half-maximal PKD activation for both CCK-8 and gastrin was achieved at 10 nM. Treatment with various concentrations of the selective PKC inhibitors Ro 31-8220 or GF-I potently blocked PKD activation induced by subsequent addition of CCK-8 in a concentration-dependent fashion. Our results indicate that PKC-dependent PKD activation is a novel early event in the action of gastrin and CCK-8 via CCK2 receptors.

【 授权许可】

Unknown