Cited by 24Receptor Mechanisms and SignalingIon Channels and ReceptorsPain Mechanisms and Treatments

Two to tango: GPCR oligomers and GPCR-TRP channel interactions in nociception

Yekkirala, Ajay S.·2013·Life Sciences

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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Crossref · 10.1016/j.lfs.2012.06.021

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Authors
Yekkirala, A. S.
Affiliations
Boston Children's Hospital (US)
Corresponding author
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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