title: Solubilization of G protein-coupled receptors: a convenient strategy to explore lipid-receptor interaction.
abstract: G protein-coupled receptors (GPCRs) are the largest class of molecules involved in signal transduction across cell membranes and are major drug targets. Since GPCRs are integral membrane proteins, their structure and function are modulated by membrane lipids. In particular, membrane cholesterol is an important lipid in the context of GPCR function. Solubilization of integral membrane proteins is a process in which the proteins and lipids in native membranes are dissociated in the presence of a suitable amphiphilic detergent. Interestingly, solubilization offers a convenient approach to monitor lipid-receptor interaction as it results in differential extents of lipid solubilization, thereby allowing to assess the role of specific lipids on receptor function. In this review, we highlight how this solubilization strategy is utilized to decipher novel information about the structural stringency of cholesterol necessary for supporting the function of the serotonin(1A) receptor. We envision that insight in GPCR-lipid interaction would result in better understanding of GPCR function in health and disease.
authors.affiliation: CSIR-Centre for Cellular and Molecular Biology, Hyderabad, India; Academy of Scientific and Innovative Research, New Delhi, India. Electronic address: amit@ccmb.res.in.
authors.forename: Amitabha
authors.initials: A
authors.lastname: Chattopadhyay
authors.affiliation: CSIR-Indian Institute of Chemical Technology, Hyderabad, India; Academy of Scientific and Innovative Research, New Delhi, India.
authors.forename: Bhagyashree D
authors.initials: BD
authors.lastname: Rao
authors.affiliation: CSIR-Centre for Cellular and Molecular Biology, Hyderabad, India.
authors.forename: Md
authors.initials: M
authors.lastname: Jafurulla
mesh_terms: D000818:Animals; D002784:Cholesterol / Q000378:metabolism; D003902:Detergents / Q000737:chemistry*; D006801:Humans; D050356:Lipid Metabolism; D008958:Models, Molecular; D044282:Receptor, Serotonin, 5-HT1A / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000302:isolation & purification* / Q000378:metabolism*; D012995:Solubility
chemical_list: D003902:Detergents; D043562:Receptors, G-Protein-Coupled; D044282:Receptor, Serotonin, 5-HT1A; D002784:Cholesterol
keywords: Cholesterol; Detergent; GPCR; Lipid–receptor interaction; Serotonin(1A) receptor; Solubilization