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Role of cholesterol in ligand binding and G-protein coupling of serotonin1A receptors solubilized from bovine hippocampus.

Abstract：

:The serotonin(1A) (5-HT(1A)) receptor is an important member of the superfamily of seven transmembrane domain G-protein-coupled receptors. We report here that solubilization of the hippocampal 5-HT(1A) receptor by the zwitterionic detergent CHAPS is accompanied by loss of membrane cholesterol which results in a reduction in specific agonist binding activity and extent of G-protein coupling. Importantly, replenishment of cholesterol to solubilized membranes using MbetaCD-cholesterol complex restores the cholesterol content of the membrane and significantly enhances the specific agonist binding activity and G-protein coupling. These novel results provide useful information on the role of cholesterol in solubilization of G-protein-coupled receptors, an important step for molecular characterization of these receptors.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Chattopadhyay A,Jafurulla M,Kalipatnapu S,Pucadyil TJ,Harikumar KG

doi

10.1016/j.bbrc.2004.12.102

subject

Has Abstract

pub_date

2005-02-25 00:00:00

pages

1036-41

issue

4

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(04)02916-X

journal_volume

327

pub_type

杂志文章

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