ArticleBritish journal of pharmacology2004
Proteinase-activated receptor-4: evaluation of tethered ligand-derived peptides as probes for receptor function and as inflammatory agonists in vivo.
Article in British journal of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 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.
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Who cites it
39 citing papers in PubMed, 115 citations in OpenAlex.
- Protease-activated receptors act as a liaison between metabolism and inflammation.Inflammopharmacology · 2026Review
- Antiplatelet Therapy.Handbook of experimental pharmacology · 2026Review
- PAR-Induced Harnessing of EZH2 to β-Catenin: Implications for Colorectal Cancer.International journal of molecular sciences · 2022Article
- Loss of Protease-Activated Receptor 4 Prevents Inflammation Resolution and Predisposes the Heart to Cardiac Rupture After Myocardial Infarction.Circulation · 2020Article
- Proteinase Activated Receptor 4 in the Jejunum of Healthy Horses and of Horses With Epiploic Hernia.Frontiers in veterinary science · 2020Article
- Using PAR4 Inhibition as an Anti-Thrombotic Approach: Why, How, and When?International journal of molecular sciences · 2019Review
- Protease-activated receptor 4 protects mice from Coxsackievirus B3 and H1N1 influenza A virus infection.Cellular immunology · 2019Article
- New Amides and Phenylpropanoid Glucosides from the Fruits of Piper retrofractum.Natural products and bioprospecting · 2019Article
- Protease-activated receptors (PARs): mechanisms of action and potential therapeutic modulators in PAR-driven inflammatory diseases.Thrombosis journal · 2019Review
- Protease Activated Receptor 4 as a Novel Modulator of Regulatory T Cell Function.Frontiers in immunology · 2019Article
- Epithelial cell adhesion efficacy of a novel peptide identified by panning on a smooth titanium surface.International journal of oral science · 2018Article
- Protease-Activated Receptor 4 (PAR4): A Promising Target for Antiplatelet Therapy.International journal of molecular sciences · 2018Review
- Protease-activated receptor 4: from structure to function and back again.British journal of pharmacology · 2016Review
- Protease-activated receptor 4 deficiency offers cardioprotection after acute ischemia reperfusion injury.Journal of molecular and cellular cardiology · 2016Article
- Novel Allosteric Modulators of G Protein-coupled Receptors.The Journal of biological chemistry · 2015Review
- Review
- Increased expression of protease-activated receptor 2 and 4 within dorsal root ganglia in a rat model of bone cancer pain.Journal of molecular neuroscience : MN · 2015Article
- New insights into protease-activated receptor 4 signaling pathways in the pathogenesis of inflammation and neuropathic pain: a literature review.Channels (Austin, Tex.) · 2015Review
- Proteinase-activated receptors (PARs) - focus on receptor-receptor-interactions and their physiological and pathophysiological impact.Cell communication and signaling : CCS · 2013Review
- Interleukin-1β increased the expression of protease-activated receptor 4 mRNA and protein in dorsal root ganglion neurons.Neurochemical research · 2013Article
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. We evaluated the ability of a number of peptides based on the tethered ligand sequences of human, rat and murine proteinase-activated receptor-4 (PAR(4)), to serve as receptor-activating probes or antagonists for bioassays carried out in vitro and for in vivo models of inflammation. 2. In a rat PAR(4)-dependent platelet aggregation assay, the relative potencies of the active sequences (AYPGKF-NH(2)>GYPGKF-NH(2)>GYPGFK-NH(2)>GFPGKP-NH(2)) were consistent with an activation of PAR(4). 3. In the aggregation assay, the reverse or partial reverse-sequence peptides (VQGPYG-NH(2), YAPGKF-NH(2) and FKGPYA-NH(2)) were inactive, while trans-cinnamoyl (Tc)-YPGKF-NH(2), Tc-APGKF-NH(2) and N-palmitoyl-SGRRYGHALR-NH(2) (pepducin P4pal-10) were antagonists. 4. However, in an endothelium-dependent NO-mediated rat aorta (RA) relaxation assay and in a gastric longitudinal muscle (LM) contraction assay, these antagonist peptides were agonists as were most other peptides, with distinct orders of potencies that differed for both the RA and LM assays and from the platelet assay. 5. We conclude that PAR(4)-derived tethered ligand peptide agonists can act at receptors other than PAR(4) and that a judicious choice of ligands is required to probe for PAR(4) function in bioassay systems and in particular for in vivo models. 6. By selecting from these peptides the ones most reliably reflecting PAR(4) activation (AYPGKF-NH(2) as a standard agonist; YAPGKF-NH(2) as a PAR(4)-inactive standard), we were able to establish an inflammatory role for the PAR(4)-activating peptides acting via a non-neurogenic mechanism in a rat paw oedema model.
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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.