ArticleJournal of medicinal chemistry2011
Potent agonists of the protease activated receptor 2 (PAR2).
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
21 citing papers in PubMed, 29 citations in OpenAlex.
- The proteinase-activated receptor-2 mediates protective immunity in early experimental leishmaniasis.Emerging microbes & infections · 2026Article
- A New Strategy in Modulating the Protease-Activated Receptor 2 (Par2) in Autoimmune Diseases.International journal of molecular sciences · 2025Review
- C781, a β-Arrestin Biased Antagonist at Protease-Activated Receptor-2 (PAR2), Displays in vivo Efficacy Against Protease-Induced Pain in Mice.The journal of pain · 2023Article
- Alternaria alternata-induced airway epithelial signaling and inflammatory responses via protease-activated receptor-2 expression.Biochemical and biophysical research communications · 2022Article
- A Role for Protease Activated Receptor Type 3 (PAR3) in Nociception Demonstrated Through Development of a Novel Peptide Agonist.The journal of pain · 2021Article
- The cellular basis of protease-activated receptor 2-evoked mechanical and affective pain.JCI insight · 2020Article
- Molecular basis for activation and biased signaling at the thrombin-activated GPCR proteinase activated receptor-4 (PAR4).The Journal of biological chemistry · 2020Article
- Transient Photoinactivation of Cell Membrane Protein Activity without Genetic Modification by Molecular Hyperthermia.ACS nano · 2019Article
- Interaction of host and Staphylococcus aureus protease-system regulates virulence and pathogenicity.Medical microbiology and immunology · 2019Review
- High Affinity Fluorescent Probe for Proteinase-Activated Receptor 2 (PAR2).ACS medicinal chemistry letters · 2019Article
- Protease-activated receptors (PARs): mechanisms of action and potential therapeutic modulators in PAR-driven inflammatory diseases.Thrombosis journal · 2019Review
- Application of Real-Time Cell Electronic Analysis System in Modern Pharmaceutical Evaluation and Analysis.Molecules (Basel, Switzerland) · 2018Review
- eIF4E Phosphorylation InfluencesFrontiers in cellular neuroscience · 2018Article
- The MNK-eIF4E Signaling Axis Contributes to Injury-Induced Nociceptive Plasticity and the Development of Chronic Pain.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2017Article
- Potent Small Agonists of Protease Activated Receptor 2.ACS medicinal chemistry letters · 2016Article
- Article
- Application of xCELLigence RTCA Biosensor Technology for Revealing the Profile and Window of Drug Responsiveness in Real Time.Biosensors · 2015Article
- Role for β-arrestin in mediating paradoxical β2AR and PAR2 signaling in asthma.Current opinion in pharmacology · 2014Review
- Lanthanide labeling of a potent protease activated receptor-2 agonist for time-resolved fluorescence analysis.Bioconjugate chemistry · 2012Article
- β-Arrestin-2 mediates the proinflammatory effects of proteinase-activated receptor-2 in the airway.Proceedings of the National Academy of Sciences of the United States of America · 2012Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Novel peptidomimetic pharmacophores to PAR(2) were designed based on the known activating peptide SLIGRL-NH(2). A set of 15 analogues was evaluated with a model cell line (16HBE14o-) that highly expresses PAR(2). Cells exposed to the PAR(2) activating peptide with N-terminal 2-furoyl modification (2-furoyl-LIGRLO-NH(2)) initiated increases in intracellular calcium concentration ([Ca(2+)](i) EC(50) = 0.84 μM) and in vitro physiological responses as measured by the xCELLigence real time cell analyzer (RTCA EC(50) = 138 nM). We discovered two selective PAR(2) agonists with comparable potency: compound 1 (2-aminothiazol-4-yl; Ca(2+) EC(50) = 1.77 μM, RTCA EC(50) = 142 nM) and compound 2 (6-aminonicotinyl; Ca(2+) EC(50) = 2.60 μM, RTCA EC(50) = 311 nM). Unlike the previously described agonist, these novel agonists are devoid of the metabolically unstable 2-furoyl modification and thus provide potential advantages for PAR(2) peptide design for in vitro and in vivo studies. The novel compounds described herein also serve as a starting point for structure-activity relationship (SAR) design and are, for the first time, evaluated via a unique high throughput in vitro physiological assay. Together these will lead to discovery of more potent agonists and antagonists of PAR(2).
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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.