Heteromerization of G protein-coupled receptors: relevance to neurological disorders and neurotherapeutics.

CNS & Neurological Disorders Drug Targets
Laura AlbizuStuart C Sealfon

Abstract

Because G protein-coupled receptors (GPCRs) are numerous, widely expressed and involved in major physiological responses, they represent a relevant therapeutic target for drug discovery, particularly regarding pharmacological treatments of neurological disorders. Among the biological phenomena regulating receptor function, GPCR heteromerization is an important emerging area of interest and investigation. There is increasing evidence showing that heteromerization contributes to the pharmacological heterogeneity of GPCRs by modulating receptor ontogeny, activation and recycling. Although in many cases the physiological relevance of receptor heteromerization has not been fully established, the unique pharmacological and functional properties of heteromers are likely to lead to new strategies in clinical medicine. This review describes the main GPCR heteromers and their implications for major neurological disorders such as Parkinson's disease, schizophrenia and addiction. A better understanding of molecular mechanisms underlying drug interactions related to the targeting of receptor heteromers could provide more specific and efficient therapeutic agents for the treatment of brain diseases.

Citations

Aug 2, 2011·Biological Reviews of the Cambridge Philosophical Society·Skirmantas Janušonis
May 31, 2011·Molecular Brain·Javier González-Maeso
Jun 22, 2012·Expert Opinion on Drug Discovery·Linjie ChenNaiming Zhou
Jun 8, 2011·Neuropharmacology·Laura AlbizuStuart C Sealfon
Sep 10, 2013·Chemical Biology & Drug Design·Martha C Contreras-RomoJosé Correa-Basurto
May 3, 2016·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·S LiebJ Wegener
May 7, 2016·Journal of Molecular Endocrinology·Gunnar KleinauHeike Biebermann
Mar 29, 2013·International Journal of Molecular Sciences·Elmar PeschkeEckhard Mühlbauer
Jan 11, 2020·Neurotherapeutics : the Journal of the American Society for Experimental NeuroTherapeutics·Jérémie NeastaSami Ben Hamida
Apr 11, 2020·International Journal of Molecular Sciences·Ujendra Kumar, Sneha Singh
Sep 7, 2018·Frontiers in Cellular Neuroscience·Md Ezazul HaqueDong-Kug Choi
Nov 5, 2019·Frontiers in Molecular Neuroscience·Matthieu ColomLuc Zimmer
Nov 17, 2020·Frontiers in Cellular Neuroscience·Jon DelaCuesta-BarrutiaAmaia M Erdozain

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