ArticleFrontiers in endocrinology2013
Interaction of Protease-Activated Receptor 2 with G Proteins and β-Arrestin 1 Studied by Bioluminescence Resonance Energy Transfer.
Article in Frontiers in endocrinology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 25 citations in OpenAlex.
- 1-Piperidine Propionic Acid Inhibits PAR2/SerpinB3 Signaling and Reduces Glioblastoma Tumor Aggressiveness.International journal of molecular sciences · 2026Article
- Pharmacologic Modulation of the PAR-2-ERK Axis by Statins Converts Inflammatory Survival Signalling into Apoptosis in Colorectal Cancer Cells.International journal of molecular sciences · 2026Article
- Structural basis for the activation of proteinase-activated receptors PAR1 and PAR2.Nature communications · 2025Article
- Update on protease-activated receptor 2 in inflammatory and autoimmune dermatological diseases.Frontiers in immunology · 2024Review
- Discovery of Ghrelin(1-8) Analogues with Improved Stability and Functional Activity for PET Imaging.ACS pharmacology & translational science · 2023Article
- Protease-activated receptors in health and disease.Physiological reviews · 2023Review
- GαFrontiers in cell and developmental biology · 2022Review
- The PAR2 inhibitor I-287 selectively targets GαCommunications biology · 2020Article
- Role of the Helix-8 and C-Terminal Tail in Regulating Proteinase Activated Receptor 2 Signaling.ACS pharmacology & translational science · 2020Article
- Macrophage TLR4 and PAR2 Signaling: Role in Regulating Vascular Inflammatory Injury and Repair.Frontiers in immunology · 2020Review
- Systematic protein-protein interaction mapping for clinically relevant human GPCRs.Molecular systems biology · 2017Article
- Antagonism of the proinflammatory and pronociceptive actions of canonical and biased agonists of protease-activated receptor-2.British journal of pharmacology · 2016Article
- Protease-activated receptors in hemostasis.Blood · 2016Review
- Neutrophil Elastase Activates Protease-activated Receptor-2 (PAR2) and Transient Receptor Potential Vanilloid 4 (TRPV4) to Cause Inflammation and Pain.The Journal of biological chemistry · 2015Article
- Transmembrane signal transduction by peptide hormones via family B G protein-coupled receptors.Frontiers in pharmacology · 2015Review
- Endothelin-1/endothelin A receptor-mediated biased signaling is a new player in modulating human ovarian cancer cell tumorigenesis.Cellular signalling · 2014Article
- Poly(Ethylene glycol)-based backbones with high peptide loading capacities.Molecules (Basel, Switzerland) · 2014Article
- Cathepsin S causes inflammatory pain via biased agonism of PAR2 and TRPV4.The Journal of biological chemistry · 2014Article
- Comment on "The Use of BRET to Study Receptor-Protein Interactions".Frontiers in endocrinology · 2014Article
- Biased signaling of protease-activated receptors.Frontiers in endocrinology · 2014Review
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
G protein-coupled receptors are well recognized as being able to activate several signaling pathways through the activation of different G proteins as well as other signaling proteins such as β-arrestins. Therefore, understanding how such multiple GPCR-mediated signaling can be integrated constitute an important aspect. Here, we applied bioluminescence resonance energy transfer (BRET) to shed more light on the G protein coupling profile of trypsin receptor, or protease-activated receptor 2 (PAR2), and its interaction with β-arrestin1. Using YFP and Rluc fusion constructs expressed in COS-7 cells, BRET data revealed a pre-assembly of PAR2 with both Gαi1 and Gαo and a rapid and transient activation of these G proteins upon receptor activation. In contrast, no pre-assembly of PAR2 with Gα12 could be detected and their physical association can be measured with a very slow and sustained kinetics similar to that of β-arrestin1 recruitment. These data demonstrate the coupling of PAR2 with Gαi1, Gαo, and Gα12 in COS-7 cells with differences in the kinetics of GPCR-G protein coupling, a parameter that very likely influences the cellular response. Moreover, this further illustrates that pre-assembly or agonist-induced G protein interaction depends on receptor-G protein pairs indicating another level of complexity and regulation of the signaling of GPCR-G protein complexes and its multiplicity.
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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.