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      G Protein–Coupled Receptor Heteromers

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          Abstract

          G protein–coupled receptors (GPCRs) compose one of the largest families of membrane proteins involved in intracellular signaling. They are involved in numerous physiological and pathological processes and are prime candidates for drug development. Over the past decade, an increasing number of studies have reported heteromerization between GPCRs. Many investigations in heterologous systems have provided important indications of potential novel pharmacology; however, the physiological relevance of these findings has yet to be established with endogenous receptors in native tissues. In this review, we focus on family A GPCRs and describe the techniques and criteria to assess their heteromerization. We conclude that advances in approaches to study receptor complex functionality in heterologous systems, coupled with techniques that enable specific examination of native receptor heteromers in vivo, are likely to establish GPCR heteromers as novel therapeutic targets.

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          Author and article information

          Contributors
          Journal
          7607088
          673
          Annu Rev Pharmacol Toxicol
          Annu. Rev. Pharmacol. Toxicol.
          Annual review of pharmacology and toxicology
          0362-1642
          1545-4304
          5 December 2016
          22 October 2015
          2016
          09 December 2016
          : 56
          : 403-425
          Affiliations
          [1 ]Department of Pharmacology and Systems Therapeutics, Icahn School of Medicine at Mount Sinai, New York, NY 10029
          [2 ]Biologie et Bioinformatique des Systèmes de Signalisation (BIOS) Group, INRA, UMR85, Unité Physiologie de la Reproduction et des Comportements; CNRS, UMR7247, F-37380 Nouzilly, France
          [3 ]LE STUDIUM Loire Valley Institute for Advanced Studies, F-45000 Orleans, France
          [4 ]Molecular Endocrinology and Pharmacology, Harry Perkins Institute of Medical Research, Nedlands, Western Australia 6009, Australia
          [5 ]Centre for Medical Research, The University of Western Australia, Crawley, Western Australia 6009, Australia
          [6 ]Dimerix Bioscience Limited, Nedlands, Western Australia 6009, Australia
          Author notes
          [7]

          Current address: Department of Frontier Life Sciences, Nagasaki University, Nagasaki City, Nagasaki Prefecture 852-8588, Japan

          Article
          PMC5147582 PMC5147582 5147582 nihpa833704
          10.1146/annurev-pharmtox-011613-135952
          5147582
          26514203
          89da1e82-0722-4c86-97f0-34ad0f871435
          History
          Categories
          Article

          dimerization,oligomers,proximity-based assays,biochemical fingerprint,heterodimerization,bivalent ligands,allosterism

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