Bromoacetylalprenololmenthane binding to β‐receptors modulates the rate of hormone‐induced internalization but not desensitization in S49 cells

FEBS Letters

Staehelin, Matthys¹  Box, Rainer-Joachim¹ 

[1] Department Forschung, Universitätskliniken Kantonsspital, Hebelstr. 20, CH-4031 Basel, Switzerland

关键词: β-Adrenergic receptor;    Desensitization;    Receptor internalization;    Internalization blockade;    (S49 wild type cell);    BAAM;    bromoacetylalprenololmenthane;    CGP-12177;    4-(3-tert-butylamino-2-hydroxypropoxy)benzimidazole-2-one hydrochloride;    DMEM;    Dulbecco's modified Eagle's medium;    IPR;    (−)-iso-proterenol;   

DOI  :  10.1016/0014-5793(87)80079-0

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Bromoacetylalprenololmenthane was found to inhibit hormone-induced β-adrenergic receptor internalization in a dose-dependent fashion in S49 lymphoma cells, besides its known ability to bind to β-receptors irreversibly. This new found property of BAAM⁺ was taken advantage of in studying whether receptor internalization is a necessary step in the desensitization of adenylate cyclase. BAAM-treated cells showed functional desensitization even when receptor internalization had been blocked substantially by 50–65% This finding suggests that receptor internalization is not directly involved in desensitization.

【 授权许可】

Unknown