EFFECTS OF THE SELECTIVE PROTEIN-KINASE-C INHIBITOR RO-31-7549 ON HUMAN ANGIOTENSIN-II RECEPTOR DESENSITIZATION AND INTRACELLULAR CALCIUM-RELEASE

被引：16

作者：

BARKER, S

KAPAS, S

FLUCK, RJ

CLARK, AJL

机构：

[1] ST BARTHOLOMEWS HOSP,COLL MED,DEPT CHEM ENDOCRINOL,MOLEC ENDOCRINOL LAB,LONDON EC1A 7BE,ENGLAND

[2] ST BARTHOLOMEWS HOSP,COLL MED,DEPT NEPHROL,LONDON EC1A 7BE,ENGLAND

来源：

FEBS LETTERS | 1995年 / 369卷 / 2-3期

关键词：

ANGIOTENSIN RECEPTOR; DESENSITIZATION; PROTEIN KINASE C; CALCIUM RELEASE; FURA; 2; CHO CELL;

D O I：

10.1016/0014-5793(95)00725-O

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The mechanism underlying type I angiotensin II (Ang II) receptor (AT1 receptor) desensitisation is unknown. Structural features suggest it may be a substrate for protein kinase C (PKC). The effects of a selective PKC inhibitor, Ro 31-7539, on receptor desensitisation were investigated in CHO cells expressing the human AT1 receptor. Desensitisation was demonstrated with respect to the calcium response to Ang II in Fura-2-loaded cells. Ro 31-7549 had no effect on desensitisation. However, pretreatment with Ro 31-7519 caused a dose-dependent reduction in calcium release from intracellular stores. PKC may therefore act at a locus distal from the receptor itself.

引用

页码：263 / 266

页数：4

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