ArticleThe Biochemical journal2008
CXCR2 chemokine receptor antagonism enhances DOP opioid receptor function via allosteric regulation of the CXCR2-DOP receptor heterodimer.
Article in The Biochemical journal, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
33 citing papers in PubMed, 74 citations in OpenAlex.
- Safety and tolerability of low-dose naltrexone therapy in children with moderate to severe Crohn's disease: a pilot study.Journal of clinical gastroenterology · 2013Trial
- Dual CCR2/CCR5 Antagonism with Cenicriviroc Alleviates Nerve Injury-Induced Hypersensitivity and Prevents Morphine Tolerancevia Modulation of Neuroimmune Signaling.Cellular and molecular neurobiology · 2026Article
- Article
- Pharmacological Blockade of Spinal CXCL3/CXCR2 Signaling by NVP CXCR2 20, a Selective CXCR2 Antagonist, Reduces Neuropathic Pain Following Peripheral Nerve Injury.Frontiers in immunology · 2019Article
- A guide to chemokines and their receptors.The FEBS journal · 2018Review
- Molecular details of dimerization kinetics reveal negligible populations of transient µ-opioid receptor homodimers at physiological concentrations.Scientific reports · 2018Article
- Effect of CXCR2 Inhibition on Behavioral Outcomes and Pathology in Rat Model of Neuromyelitis Optica.Journal of immunology research · 2018Article
- Orphan GPR61, GPR62 and GPR135 receptors and the melatonin MTScientific reports · 2017Article
- Mechanisms of Regulation of the Chemokine-Receptor Network.International journal of molecular sciences · 2017Review
- Role of the CXCL8-CXCR1/2 Axis in Cancer and Inflammatory Diseases.Theranostics · 2017Review
- Molecular Pharmacology of δ-Opioid Receptors.Pharmacological reviews · 2016Review
- The triplet puzzle theory indicates extensive formation of heteromers between opioid and chemokine receptor subtypes.Journal of neural transmission (Vienna, Austria : 1996) · 2015Article
- In vivo opioid receptor heteromerization: where do we stand?British journal of pharmacology · 2015Review
- Chemokine receptor oligomerization and allostery.Progress in molecular biology and translational science · 2013Review
- Arrest Functions of the MIF Ligand/Receptor Axes in Atherogenesis.Frontiers in immunology · 2013Article
- Identification and profiling of novel α1A-adrenoceptor-CXC chemokine receptor 2 heteromer.The Journal of biological chemistry · 2012Article
- Pharmacological modulation of chemokine receptor function.British journal of pharmacology · 2012Review
- Cys-27 variant of human δ-opioid receptor modulates maturation and cell surface delivery of Phe-27 variant via heteromerization.The Journal of biological chemistry · 2012Article
- Evidence for activity-regulated hormone-binding cooperativity across glycoprotein hormone receptor homomers.Nature communications · 2012Article
- CXCR2 in acute lung injury.Mediators of inflammation · 2012Review
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3 authors at 1 institution in 1 country.
Funding
Abstract
Opioid agonists have a broad range of effects on cells of the immune system, including modulation of the inflammatory response, and opioid and chemokine receptors are co-expressed by many white cells. Hetero-oligomerization of the human DOP opioid and chemokine CXCR2 receptors could be detected following their co-expression by each of co-immunoprecipitation, three different resonance energy transfer techniques and the construction of pairs of individually inactive but potentially complementary receptor G-protein alpha subunit fusion proteins. Although DOP receptor agonists and a CXCR2 antagonist had no inherent affinity for the alternative receptor when either receptor was expressed individually, use of cells that expressed a DOP opioid receptor construct constitutively, and in which expression of a CXCR2 receptor construct could be regulated, demonstrated that the CXCR2 antagonist enhanced the function of DOP receptor agonists only in the presence of CXCR2. This effect was observed for both enkephalin- and alkaloid-based opioid agonists, and the effective concentrations of the CXCR2 antagonist reflected CXCR2 receptor occupancy. Entirely equivalent results were obtained in cells in which the native DOP opioid receptor was expressed constitutively and in which expression of the isolated CXCR2 receptor could be induced. These results indicate that a CXCR2 receptor antagonist can enhance the function of agonists at a receptor for which it has no inherent direct affinity by acting as an allosteric regulator of a receptor that is a heterodimer partner for the CXCR2 receptor. These results have novel and important implications for the development and use of small-molecule therapeutics.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.