G Protein-Coupled Receptor Heteromers

Ivone Gomes, Mohammed Akli Ayoub, Wakako Fujita, Werner C. Jaeger, Kevin D.G. Pfleger, Lakshmi A. Devi

Research output: Contribution to journalArticlepeer-review

216 Scopus citations


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.

Original languageEnglish
Pages (from-to)403-425
Number of pages23
JournalAnnual Review of Pharmacology and Toxicology
StatePublished - 6 Jan 2016


  • Allosterism
  • Biochemical fingerprint
  • Bivalent ligands
  • Dimerization
  • Heterodimerization
  • Oligomers
  • Proximity-based assays


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