G protein-coupled receptor heteromers
Open accessAbstract
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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An increase in the BRET signal after OXT and quinpirole co-stimulation could also be explained by co-location/co-presence of OXTR and D2R in small endocytic vesicles, but this is considered less likely.
“An increase in the BRET signal after OXT and quinpirole co-stimulation could also be explained by the co-location/co-presence of OXTR and D2R in small endocytic vesicles (Gomes et al., 2016). However, while this possibility cannot be excluded, it is considered less likely in view of the experimental data reported previously (Romero-Fernandez et al., 2013).”
From Evidence for the existence of facilitatory interactions between the dopamine D2 receptor and the oxytocin receptor in the amygdala of the rat relevance for anxiolytic actions (2023) · cites this paper as Gomes et al., 2016
Co-location/co-presence of OXTR and D2R in small endocytic vesicles is a less likely explanation for the increase in BRET signal after OXT and quinpirole co-stimulation.
“An increase in the BRET signal after OXT and quinpirole co-stimulation could also be explained by the co-location/co-presence of OXTR and D2R in small endocytic vesicles (Gomes et al., 2016). However, while this possibility cannot be excluded, it is considered less likely in view of the experimental data reported previously (Romero-Fernandez et al., 2013).”
From Evidence for the existence of facilitatory interactions between the dopamine D2 receptor and the oxytocin receptor in the amygdala of the rat relevance for anxiolytic actions (2023) · cites this paper as Gomes et al., 2016
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References 255 · Cited by 262
- Authors
- Gomes, I., Ayoub, M. A., Fujita, W., Jaeger, W. C., Pfleger, K. D. G., & Devi, L. A.
- Affiliations
- Icahn School of Medicine at Mount Sinai (US)
- Centre National de la Recherche Scientifique (FR)
- Nagasaki University (JP)
- The University of Western Australia (AU)
- Venue
- Annual Review of Pharmacology and Toxicology
- Publisher
- Annual Reviews
- Published
- 2016-01-06
- Volume
- 56
- Issue
- 1
- Pages
- 403-425
- ISSN
- 0362-1642 (ISSN-L)
- 1545-4304
- PMC
- PMC5147582
- OpenAlex
- W2165408834
- Cited by
- 262
- References
- 255
- Citations by year
- 2026: 6 · 2025: 15 · 2024: 19 · 2023: 19 · 2022: 22 · 2021: 27 · 2020: 29 · 2019: 47 · 2018: 36 · 2017: 24 · 2016: 17 · 2015: 1
- FWCI
- 2.52
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- The Annual Review of Pharmacology and Toxicology (publishedVersion)
- UWA Profiles and Research Repository (UWA) (publishedVersion, other-oa)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- HAL (submittedVersion)
- Funders
- National Institutes of Health (DA 008863, NS026880)
- Medical Research Council
- Australian Research Council (DP120101297, FT100100271)
- National Health and Medical Research Council (1085842)
- National Institute on Drug Abuse (DA008863, R56DA008863, R37DA008863, R01DA008863)
- National Institute of Neurological Disorders and Stroke (R01NS026880, NS-026880)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Keywords
- G protein-coupled receptors, receptor heteromers, heterologous expression systems, intracellular signaling, therapeutic target, drug development
- MeSH terms
- Animals, Humans, Membrane Proteins, Signal Transduction, Receptors, G-Protein-Coupled, Drug Discovery
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