G Protein–Coupled Receptor Heteromers
Identifieur interne : 002C89 ( Ncbi/Curation ); précédent : 002C88; suivant : 002C90G Protein–Coupled Receptor Heteromers
Auteurs : Ivone Gomes [États-Unis] ; Mohammed Akli Ayoub [France] ; Wakako Fujita [États-Unis] ; Werner C. Jaeger [Australie] ; Kevin D. G. Pfleger [Australie] ; Lakshmi A. Devi [États-Unis]Source :
- Annual review of pharmacology and toxicology [ 0362-1642 ] ; 2015.
Descripteurs français
- KwdFr :
- MESH :
- métabolisme : Protéines membranaires, Récepteurs couplés aux protéines G.
- physiologie : Transduction du signal.
- Animaux, Découverte de médicament, Humains.
English descriptors
- KwdEn :
- MESH :
- chemical , metabolism : Membrane Proteins, Receptors, G-Protein-Coupled.
- methods : Drug Discovery.
- physiology : Signal Transduction.
- Animals, Humans.
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.
Url:
DOI: 10.1146/annurev-pharmtox-011613-135952
PubMed: 26514203
PubMed Central: 5147582
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PMC:5147582Le document en format XML
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<front><div type="abstract" xml:lang="en"><p id="P1">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.</p>
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