Two to tango: GPCR oligomers and GPCR-TRP channel interactions in nociception
Abstract
G protein coupled receptors (GPCRs) represent the largest family of cell surface receptors that are involved in regulating several physiological and behavioral responses in organisms. Indeed, over half of all the approved drugs on the market target GPCRs. Over the past twenty years, several lines of evidence have suggested that GPCRs associate to form oligomeric structures that substantially expand the complexity of signaling processes in vivo. In addition, GPCRs have also been shown to functionally regulate ion channels and help fine-tune neurotransmission. In this review, we will discuss recent advances in both mechanisms, with specific focus on opioid receptors, cannabinoid receptors and transient receptor potential (TRP) calcium channels in nociception. A better understanding of such mechanisms will be imperative in designing analgesics devoid of deleterious side effects and mitigating drug abuse.
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GPCRs directly or indirectly modulate several TRP channels.
“GPCRs directly or indirectly modulate several TRP channels [44,45].”
From G-protein-coupled receptor participates in 20-hydroxyecdysone signaling on the plasma membrane (2014) · cites this paper as [45]
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From Atomic Structures to Neuronal Functions of G Protein–Coupled Receptors
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“Opioid receptors form complexes with transient receptor potential (TRP) Ca2+ channels as well (Yekkirala 2013).”
BackgroundG-protein-coupled receptor participates in 20-hydroxyecdysone signaling on the plasma membrane
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- Authors
- Yekkirala, A. S.
- Affiliations
- Boston Children's Hospital (US)
- Corresponding author
- Yekkirala, Ajay S.
- ORCID
- Yekkirala, Ajay S.
- Venue
- Life Sciences
- Publisher
- Elsevier BV
- Published
- 2013-03
- Volume
- 92
- Issue
- 8-9
- Pages
- 438-445
- ISSN
- 0024-3205 (ISSN-L)
- OpenAlex
- W2067666520
- Cited by
- 24
- References
- 127
- Citations by year
- 2026: 1 · 2024: 4 · 2021: 3 · 2020: 4 · 2019: 3 · 2018: 1 · 2017: 2 · 2016: 2 · 2014: 2 · 2013: 2
- FWCI
- 0.12
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Life Sciences (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
- Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
- Keywords
- G protein-coupled receptors, nociception, opioid receptors, cannabinoid receptors, TRP channels, ion channel modulation, analgesic drug design, drug abuse
- MeSH terms
- Analgesics, Animals, Humans, Ligands, Receptors, Opioid, Receptors, G-Protein-Coupled, Receptors, Cannabinoid, Transient Receptor Potential Channels, Nociception
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