INTERNALIZATION OF THE RAT AT(1A) AND AT(1B) RECEPTORS - PHARMACOLOGICAL AND FUNCTIONAL REQUIREMENTS

被引:92
作者
CONCHON, S [1 ]
MONNOT, C [1 ]
TEUTSCH, B [1 ]
CORVOL, P [1 ]
CLAUSER, E [1 ]
机构
[1] COLL FRANCE,INSERM,U36,F-75005 PARIS,FRANCE
关键词
ANGIOTENSIN II; G-PROTEIN COUPLED RECEPTOR; INTERNALIZATION;
D O I
10.1016/0014-5793(94)00703-9
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 capacity of the angiotensin II (AngII) agonist [Sar1]AngII, the antagonist [Sar1-Ile8]AngII and the non-peptidic antagonist DuP753 to undergo receptor internalization were studied in Chinese hamster ovary cells expressing rat AngII type 1a or 1b receptors (AT(1a) or AT(1b)) or a mutant of AT(1a) (Asn(74)) unable to couple G-protein. In this expression system, the ligand-induced internalization of rat AT(1a) and AT(1b) are similar. Moreover, peptidic ligands, either the agonist or antagonist, induce a significant internalization of AT(1) receptors, but the non-peptidic antagonist DuP753 is far less potent. Finally, the normal internalization of the mutant Asn(74) demonstrates that receptor activation and G-protein coupling are not required for AT(1a) internalization.
引用
收藏
页码:365 / 370
页数:6
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