Role of cholesterol in ligand binding and G-protein coupling of serotonin1A receptors solubilized from bovine hippocampus |
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Authors: | Chattopadhyay Amitabha Jafurulla Md Kalipatnapu Shanti Pucadyil Thomas J Harikumar Kaleeckal G |
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Institution: | Centre for Cellular and Molecular Biology, Uppal Road, Hyderabad 500 007, India. amit@ccmb.res.in |
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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. |
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Keywords: | Serotonin1A receptor Solubilization Cholesterol CHAPS G-protein coupling |
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