Disease-specific heteromerization of G-protein-coupled receptors that target drugs of abuse

Ivone Gomes, Wakako Fujita, Moraje V. Chandrakala, Lakshmi A. Devi

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

31 Scopus citations


Drugs of abuse such as morphine or marijuana exert their effects through the activation of G-protein-coupled receptors (GPCRs), the opioid and cannabinoid receptors, respectively. Moreover, interactions between either of these receptors have been shown to be involved in the rewarding effects of drugs of abuse. Recent advances in the field, using a variety of approaches, have demonstrated that many GPCRs, including opioid, cannabinoid, and dopamine receptors, can form associations between different receptor subtypes or with other GPCRs to form heteromeric complexes. The formation of these complexes, in turn, leads to the modulation of the properties of individual protomers. The development of tools that can selectively disrupt GPCR heteromers as well as monoclonal antibodies that can selectively block signaling by specific heteromer pairs has indicated that heteromers involving opioid, cannabinoid, or dopamine receptors may play a role in various disease states. In this review, we describe evidence for opioid, cannabinoid, and dopamine receptor heteromerization and the potential role of GPCR heteromers in pathophysiological conditions.

Original languageEnglish
Title of host publicationOligomerization in Health and Disease
PublisherElsevier B.V.
Number of pages59
ISBN (Print)9780123869319
StatePublished - 2013

Publication series

NameProgress in Molecular Biology and Translational Science
ISSN (Print)1877-1173


  • Cannabinoids
  • Dimerization
  • Dopamine
  • G-protein-coupled receptors
  • Morphine
  • Oligomerization
  • Opioids


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