Separation of the structural requirements for agonist-promoted activation and sequestration of the beta-adrenergic receptor.

Separation of the structural requirements for agonist-promoted activation and sequestration of the beta-adrenergic receptor.
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分离激动剂促进的β-肾上腺素受体激活和隔离的结构要求。

DOI:
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发表时间:
1990
影响因子:
3.6
通讯作者:
C. Strader
C. Strader
中科院分区:
医学3区
文献类型:
--
作者:
A. Cheung;R. A. Dixon;W. Hill;I. Sigal;C. Strader

文献摘要

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The deletion of residues 222-229 from the hamster beta 2-adrenergic receptor (beta AR) resulted in an inability of the mutant receptor to couple to the guanine nucleotide-binding protein (G protein) Gs and to undergo the agonist-mediated sequestration response that is associated with desensitization [Mol. Pharmacol. 34:132-138 (1989)]. Replacement of this region of the beta AR with the analogous region of the M1-muscarinic acetylcholine receptor restored the sequestration response but not the G protein activation. These data suggest that there is a structural, rather than a functional, relationship between these two processes and demonstrate that G protein coupling is not a prerequisite for receptor sequestration.