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

Amitabha Chattopadhyay, Md Jafurulla, Shanti Kalipatnapu, Thomas J. Pucadyil, Kaleeckal G. Harikumar

Research output: Contribution to journalArticle

37 Scopus citations

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 languageEnglish (US)
Pages (from-to)1036-1041
Number of pages6
JournalBiochemical and Biophysical Research Communications
Volume327
Issue number4
DOIs
StatePublished - Feb 25 2005

Keywords

  • CHAPS
  • Cholesterol
  • G-protein coupling
  • Serotonin receptor
  • Solubilization

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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