ArticleThe Journal of biological chemistry2012
Identification and profiling of novel α1A-adrenoceptor-CXC chemokine receptor 2 heteromer.
Article in The Journal of biological chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 50 citations in OpenAlex.
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- αInternational journal of molecular sciences · 2023Review
- αProceedings of the National Academy of Sciences of the United States of America · 2022Article
- Novel Pharmacology Following Heteromerization of the Angiotensin II Type 2 Receptor and the Bradykinin Type 2 Receptor.Frontiers in endocrinology · 2022Article
- GPCR heteromers: An overview of their classification, function and physiological relevance.Frontiers in endocrinology · 2022Review
- Profiling novel pharmacology of receptor complexes using Receptor-HIT.Biochemical Society transactions · 2021Review
- UDP-glucose and P2Y14 receptor amplify allergen-induced airway eosinophilia.The Journal of clinical investigation · 2021Article
- Investigation of Receptor Heteromers Using NanoBRET Ligand Binding.International journal of molecular sciences · 2021Article
- Interplay Between Angiotensin II Type 1 Receptor and Thrombin Receptor Revealed by Bioluminescence Resonance Energy Transfer Assay.Frontiers in pharmacology · 2020Article
- Coupling to Gq Signaling Is Required for Cardioprotection by an Alpha-1A-Adrenergic Receptor Agonist.Circulation research · 2019Article
- Arrestin recruitment and signaling by G protein-coupled receptor heteromers.Neuropharmacology · 2019Review
- What makes the αBritish journal of pharmacology · 2019Review
- Constraints on GPCR Heterodimerization Revealed by the Type-4 Induced-Association BRET Assay.Biophysical journal · 2019Article
- Transactivation of RAGE mediates angiotensin-induced inflammation and atherogenesis.The Journal of clinical investigation · 2019Article
- Heterologous phosphorylation-induced formation of a stability lock permits regulation of inactive receptors by β-arrestins.The Journal of biological chemistry · 2018Article
- Article
- Mechanisms of Regulation of the Chemokine-Receptor Network.International journal of molecular sciences · 2017Review
- Apelin receptor homodimer-oligomers revealed by single-molecule imaging and novel G protein-dependent signaling.Scientific reports · 2017Article
- New Insights into Mechanisms and Functions of Chemokine (C-X-C Motif) Receptor 4 Heteromerization in Vascular Smooth Muscle.International journal of molecular sciences · 2016Article
- G Protein-Coupled Receptor Heteromers.Annual review of pharmacology and toxicology · 2016Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We have provided the first evidence for specific heteromerization between the α(1A)-adrenoceptor (α(1A)AR) and CXC chemokine receptor 2 (CXCR2) in live cells. α(1A)AR and CXCR2 are both expressed in areas such as the stromal smooth muscle layer of the prostate. By utilizing the G protein-coupled receptor (GPCR) heteromer identification technology on the live cell-based bioluminescence resonance energy transfer (BRET) assay platform, our studies in human embryonic kidney 293 cells have identified norepinephrine-dependent β-arrestin recruitment that was in turn dependent upon co-expression of α(1A)AR with CXCR2. These findings have been supported by co-localization observed using confocal microscopy. This norepinephrine-dependent β-arrestin recruitment was inhibited not only by the α(1)AR antagonist Terazosin but also by the CXCR2-specific allosteric inverse agonist SB265610. Furthermore, Labetalol, which is marketed for hypertension as a nonselective β-adrenoceptor antagonist with α(1)AR antagonist properties, was identified as a heteromer-specific-biased agonist exhibiting partial agonism for inositol phosphate production but essentially full agonism for β-arrestin recruitment at the α(1A)AR-CXCR2 heteromer. Finally, bioluminescence resonance energy transfer studies with both receptors tagged suggest that α(1A)AR-CXCR2 heteromerization occurs constitutively and is not modulated by ligand. These findings support the concept of GPCR heteromer complexes exhibiting distinct pharmacology, thereby providing additional mechanisms through which GPCRs can potentially achieve their diverse biological functions. This has important implications for the use and future development of pharmaceuticals targeting these receptors.
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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.