RAPID AND REVERSIBLE UNCOUPLING OF THE HEPATIC ALPHA(1)-ADRENERGIC RECEPTOR AND GUANINE-NUCLEOTIDE-BINDING PROTEIN BY PHORBOL 12,13-DIBUTYRATE

被引：7

作者：

BEELER, JF ^{[1
]}

COOPER, RH ^{[1
]}

机构：

[1] UNIV S CAROLINA,SCH MED,DEPT PHARMACOL,COLUMBIA,SC 29208

来源：

BIOCHIMICA ET BIOPHYSICA ACTA | 1993年 / 1176卷 / 03期

关键词：

PHORBOL ESTER; ADRENERGIC RECEPTOR; ALPHA(1)-; G-PROTEIN; RECEPTOR DESENSITIZATION; HEPATOCYTE; (RAT);

D O I：

10.1016/0167-4889(93)90064-V

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：

Phorbol 12,13-dibutyrate (PDBU), 1 mug/ml for 2 min, abolished alpha1-adrenergic receptor (AR)-mediated signal transduction in rat hepatocytes and converted 100% of alpha1-ARs to a low-affinity state, similar to effects of a non-hydrolyzable GTP analog. Reversal of PDBU inhibition restored high-affinity alpha1-ARs towards control values. The rapid uncoupling of the alpha1-AR and guanine-nucleotide-binding protein by PDBU, and reversibility associated with reactivation of alpha1-adrenergic signaling, identify this as an important inhibitory locus for PDBU.

引用

页码：339 / 342

页数：4

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