Revolution in GPCR signalling: opioid receptor heteromers as novel therapeutic targets: IUPHAR Review 10

作者: Wakako Fujita , Ivone Gomes , Lakshmi A Devi

DOI: 10.1111/BPH.12798

关键词: CannabinoidPharmacologyOpioidG protein-coupled receptorHeteromerMetabotropic receptorNeuroscienceReceptorRhodopsin-like receptorsOpioid receptorChemistry

摘要: GPCRs can interact with each other to form homomers or heteromers. Homomers involve interactions the same receptor type while heteromers between two different GPCRs. These receptor–receptor modulate not only binding but also signalling and trafficking properties of individual receptors. Opioid heteromerization has been extensively investigated objective identifying novel therapeutic targets that are as potent morphine without side effects associated chronic use. In this context, studies have described types opioid receptors a wide range including adrenoceptors, cannabinoid, 5-HT, metabotropic glutamate sensory neuron-specific Recent advances in field involving generation heteromer-specific reagents (antibodies ligands) membrane-permeable peptides disrupt heteromer interaction helping elucidate physiological role contribution partner For example, using targeting interface implicated μ δ development tolerance morphine, gastrin-releasing peptide morphine-induced itch. addition, number ligands selectively target exhibit antinociception decrease commonly review, we summarize latest findings regarding biological functional characteristics both vitro vivo.

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