Abstract
G-protein coupled receptors (GPCRs) are the largest class of molecules involved in signal transduction across membranes, and represent major targets in the development of novel drug candidates in all clinical areas. Since GPCRs are integral membrane proteins, interaction of membrane lipids such as cholesterol and sphingolipids with GPCRs constitutes an emerging area of research in contemporary biology. Cholesterol and sphingolipids represent important lipid components of eukaryotic membranes and play a crucial role in a variety of cellular functions. In this review, we highlight the role of these vital lipids in the function of two representative GPCRs, the serotonin1A receptor and the adrenergic receptor. We believe that development in deciphering molecular details of the nature of GPCR-lipid interaction would lead to better insight into our overall understanding of GPCR function in health and disease.
Keywords: Adrenergic receptor, adenosine receptor, CRAC, cholesterol, G-protein coupled receptor, SBD, serotonin1A receptor, sphingolipids, G-protein coupled receptors (GPCRs), transduction across membranes
Current Medicinal Chemistry
Title:Membrane Lipids in the Function of Serotonin and Adrenergic Receptors
Volume: 20 Issue: 1
Author(s): Md. Jafurulla and A. Chattopadhyay
Affiliation:
Keywords: Adrenergic receptor, adenosine receptor, CRAC, cholesterol, G-protein coupled receptor, SBD, serotonin1A receptor, sphingolipids, G-protein coupled receptors (GPCRs), transduction across membranes
Abstract: G-protein coupled receptors (GPCRs) are the largest class of molecules involved in signal transduction across membranes, and represent major targets in the development of novel drug candidates in all clinical areas. Since GPCRs are integral membrane proteins, interaction of membrane lipids such as cholesterol and sphingolipids with GPCRs constitutes an emerging area of research in contemporary biology. Cholesterol and sphingolipids represent important lipid components of eukaryotic membranes and play a crucial role in a variety of cellular functions. In this review, we highlight the role of these vital lipids in the function of two representative GPCRs, the serotonin1A receptor and the adrenergic receptor. We believe that development in deciphering molecular details of the nature of GPCR-lipid interaction would lead to better insight into our overall understanding of GPCR function in health and disease.
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Jafurulla Md. and Chattopadhyay A., Membrane Lipids in the Function of Serotonin and Adrenergic Receptors, Current Medicinal Chemistry 2013; 20 (1) . https://dx.doi.org/10.2174/0929867311302010006
DOI https://dx.doi.org/10.2174/0929867311302010006 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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