ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2013
Baclofen and other GABAB receptor agents are allosteric modulators of the CXCL12 chemokine receptor CXCR4.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 44 citations in OpenAlex.
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- The role of CXCL12/CXCR4/CXCR7 axis in cognitive impairment associated with neurodegenerative diseases.Brain, behavior, & immunity - health · 2025Review
- Progress in structure-based drug development targeting chemokine receptors.Frontiers in pharmacology · 2025Review
- Role of G-protein coupled receptors in cardiovascular diseases.Frontiers in cardiovascular medicine · 2023Review
- Seizure-induced hilar ectopic granule cells in the adult dentate gyrus.Frontiers in neuroscience · 2023Review
- The Zonulin-transgenic mouse displays behavioral alterations ameliorated via depletion of the gut microbiota.Tissue barriers · 2022Article
- GABACurrent topics in behavioral neurosciences · 2022Review
- Embryonic Valproate Exposure Alters Mesencephalic Dopaminergic Neurons Distribution and Septal Dopaminergic Gene Expression in Domestic Chicks.Frontiers in integrative neuroscience · 2022Article
- The discriminatory power of the T cell receptor.eLife · 2021Article
- Opioid and chemokine regulation of cortical synaptodendritic damage in HIV-associated neurocognitive disorders.Brain research · 2019Review
- Gabapentin Is a Potent Activator of KCNQ3 and KCNQ5 Potassium Channels.Molecular pharmacology · 2018Article
- Direct neurotransmitter activation of voltage-gated potassium channels.Nature communications · 2018Article
- Activation of GABAMediators of inflammation · 2018Article
- A Review of the Potential Mechanisms of Action of Baclofen in Alcohol Use Disorder.Frontiers in psychiatry · 2018Review
- Agarose Spot as a Comparative Method for in situ Analysis of Simultaneous Chemotactic Responses to Multiple Chemokines.Scientific reports · 2017Article
- Label-free quantification of calcium-sensor targeting to photoreceptor guanylate cyclase and rhodopsin kinase by backscattering interferometry.Scientific reports · 2017Article
- Discovery and characterization of novel small-molecule CXCR4 receptor agonists and antagonists.Scientific reports · 2016Article
- Predicted molecular signaling guiding photoreceptor cell migration following transplantation into damaged retina.Scientific reports · 2016Article
- Modulation of TLR3/TLR4 inflammatory signaling by the GABAB receptor agonist baclofen in glia and immune cells: relevance to therapeutic effects in multiple sclerosis.Frontiers in cellular neuroscience · 2015Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
CXCR4, a receptor for the chemokine CXCL12 (stromal-cell derived factor-1α), is a G-protein-coupled receptor (GPCR), expressed in the immune and CNS and integrally involved in various neurological disorders. The GABAB receptor is also a GPCR that mediates metabotropic action of the inhibitory neurotransmitter GABA and is located on neurons and immune cells as well. Using diverse approaches, we report novel interaction between GABAB receptor agents and CXCR4 and demonstrate allosteric binding of these agents to CXCR4. First, both GABAB antagonists and agonists block CXCL12-elicited chemotaxis in human breast cancer cells. Second, a GABAB antagonist blocks the potentiation by CXCL12 of high-threshold Ca(2+) channels in rat neurons. Third, electrophysiology in Xenopus oocytes and human embryonic kidney cell line 293 cells in which we coexpressed rat CXCR4 and the G-protein inward rectifier K(+) (GIRK) channel showed that GABAB antagonist and agonist modified CXCL12-evoked activation of GIRK channels. To investigate whether GABAB ligands bind to CXCR4, we expressed this receptor in heterologous systems lacking GABAB receptors and performed competition binding experiments. Our fluorescent resonance energy transfer experiments suggest that GABAB ligands do not bind CXCR4 at the CXCL12 binding pocket suggesting allosteric modulation, in accordance with our electrophysiology experiments. Finally, using backscattering interferometry and lipoparticles containing only the CXCR4 receptor, we quantified the binding affinity for the GABAB ligands, confirming a direct interaction with the CXCR4 receptor. The effect of GABAergic agents on CXCR4 suggests new therapeutic potentials for neurological and immune diseases.
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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.