ArticleThe Journal of biological chemistry2010
Expression of a G protein-coupled receptor (GPCR) leads to attenuation of signaling by other GPCRs: experimental evidence for a spontaneous GPCR constitutive inactive form.
Article in The Journal of biological chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 41 citations in OpenAlex.
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- Kinetic model of partial agonism reveals cellular basis of ligand efficacy.The Journal of biological chemistry · 2026Article
- Local GPCR density tips the balance of μ-opioid receptor trafficking.bioRxiv : the preprint server for biology · 2026Article
- Identification and molecular characterization of missense mutations in orphan G protein-coupled receptor GPR61 occurring in severe obesity.Molecular pharmacology · 2025Article
- Identification of Environmental Compounds That May Trigger Early Female Puberty by Activating Human GnRHR and KISS1R.Endocrinology · 2024Article
- Detecting and measuring of GPCR signaling - comparison of human induced pluripotent stem cells and immortal cell lines.Frontiers in endocrinology · 2023Review
- Comparison of fluorescence biosensors and whole-cell patch clamp recording in detecting ACh, NE, and 5-HT.Frontiers in cellular neuroscience · 2023Article
- Propranolol blocks osteosarcoma cell cycle progression, inhibits angiogenesis and slows xenograft growth in combination with cisplatin-based chemotherapy.Scientific reports · 2022Article
- Novel inhibitors of phosphorylation independent activity of GRK2 modulate cAMP signaling.Pharmacology research & perspectives · 2022Article
- A fast, high-affinity fluorescent serotonin biosensor engineered from a tick lipocalin.Nature methods · 2021Article
- Transfection methods for high-throughput cellular assays of voltage-gated calcium and sodium channels involved in pain.PloS one · 2021Article
- Article
- Monitoring Cannabinoid CB2 -Receptor Mediated cAMP Dynamics by FRET-Based Live Cell Imaging.International journal of molecular sciences · 2020Article
- The Regulator of G Protein Signaling Homologous Domain of G Protein-Coupled Receptor Kinase 2 Mediates Short-Term Desensitization of β3-Adrenergic Receptor.Frontiers in pharmacology · 2020Article
- Exploring a New Natural Treating Agent for Primary Hypertension: Recent Findings and Forthcoming Perspectives.Journal of clinical medicine · 2019Review
- A Model of Glucocorticoid Receptor Interaction With Coregulators Predicts Transcriptional Regulation of Target Genes.Frontiers in pharmacology · 2019Article
- Receptor Quaternary Organization Explains G Protein-Coupled Receptor Family Structure.Cell reports · 2017Article
- Designed cell consortia as fragrance-programmable analog-to-digital converters.Nature chemical biology · 2017Article
- A Novel Effect of β-Adrenergic Receptor on Mammary Branching Morphogenesis and its Possible Implications in Breast Cancer.Journal of mammary gland biology and neoplasia · 2017Article
- A synthetic biology-based device prevents liver injury in mice.Journal of hepatology · 2016Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The idea of G protein-coupled receptors (GPCRs) coupling to G protein solely in their active form was abolished when it was found that certain ligands induce a G protein-coupled but inactive receptor form. This receptor form interferes with signaling of other receptors by sequestering G protein. However, the spontaneous existence of this receptor species has never been established. The aim of the present work was to evaluate the existence of the spontaneous conformation of the receptor inactively coupled to G protein able to interfere with the response of other GPCRs. According to the law of mass action, receptor overexpression should lead to increased amounts of all spontaneously occurring species. Based on this, we generated Chinese hamster ovary (CHO-K1)-derived cell lines expressing various amounts of the human histamine H2 receptor. In these systems, the signaling of other endogenously and transiently expressed GPCRs was attenuated proportionally to human H2 receptor expression levels. G protein transfection specifically reverted this attenuation, strongly suggesting hijacking of the G protein from a common pool. Similar attenuation effects were observed when the beta(2)- adrenergic receptor was overexpressed, suggesting that this is a more general phenomenon. Moreover, in human mammary MDA-MB-231 cells, a consistent increase in the response of other GPCRs was observed when endogenous expression of beta(2)-adrenergic receptor was knocked down using specific small interfering RNAs. Our findings show that GPCRs may interact with the signaling of other receptors by modulating the availability of the G protein and suggest the existence of GPCR spontaneous coupling to G proteins in an inactive form.
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