Abstract
The serotonin1A (5-HT1A) 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 MβCD-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.
Original language | English (US) |
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Pages (from-to) | 1036-1041 |
Number of pages | 6 |
Journal | Biochemical and Biophysical Research Communications |
Volume | 327 |
Issue number | 4 |
DOIs | |
State | Published - Feb 25 2005 |
Keywords
- CHAPS
- Cholesterol
- G-protein coupling
- Serotonin receptor
- Solubilization
ASJC Scopus subject areas
- Biophysics
- Biochemistry
- Molecular Biology
- Cell Biology