ArticlePharmaceuticals (Basel, Switzerland)2023
1-Piperidine Propionic Acid as an Allosteric Inhibitor of Protease Activated Receptor-2.
Article in Pharmaceuticals (Basel, Switzerland), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 9 citations in OpenAlex.
- Regulatory mechanism of the RNF168-SCCA1-MYH9 signaling axis in the response of ulcerative colitis.Journal of gastroenterology · 2026Article
- 1-Piperidine Propionic Acid Inhibits PAR2/SerpinB3 Signaling and Reduces Glioblastoma Tumor Aggressiveness.International journal of molecular sciences · 2026Article
- Inhibition of the SerpinB3/protease-activated receptor 2 axis reduces liver cancer development and affects lipid metabolism.British journal of cancer · 2026Article
- Dissecting the Spectrum of Rare BRAF Mutations in Melanoma: A Nation-Wide Study by the Italian Melanoma Intergroup (IMI).Pigment cell & melanoma research · 2026Article
- Garlic-Derived Phytochemical Candidates Predicted to Disrupt SARS-CoV-2 RBD-ACE2 Binding and Inhibit Viral Entry.Molecules (Basel, Switzerland) · 2025Article
- Harnessing Photosynthetic ATP for Whole-Cell Biocatalysis in the CyanobacteriumACS sustainable chemistry & engineering · 2025Article
- SerpinB3/Protease Activated Receptor-2 Axis Is Essential for SARS CoV-2 Infection.ACS infectious diseases · 2025Article
- 1-Piperidine Propionic Acid Protects from Septic Shock Through Protease Receptor 2 Inhibition.International journal of molecular sciences · 2024Article
- Inhibition of Protease-Activated Receptor-2 Activation in Parkinson's Disease Using 1-Piperidin Propionic Acid.Biomedicines · 2024Article
- Protease activated receptor 2 as a novel druggable target for the treatment of metabolic dysfunction-associated fatty liver disease and cancer.Frontiers in immunology · 2024Review
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In the last decades, studies on the inflammatory signaling pathways in multiple pathological contexts have revealed new targets for novel therapies. Among the family of G-protein-coupled Proteases Activated Receptors, PAR2 was identified as a driver of the inflammatory cascade in many pathologies, ranging from autoimmune disease to cancer metastasis. For this reason, many efforts have been focused on the development of potential antagonists of PAR2 activity. This work focuses on a small molecule, 1-Piperidine Propionic Acid (1-PPA), previously described to be active against inflammatory processes, but whose target is still unknown. Stabilization effects observed by cellular thermal shift assay coupled to in-silico investigations, including molecular docking and molecular dynamics simulations, suggested that 1-PPA binds PAR2 in an allosteric pocket of the receptor inactive conformation. Functional studies revealed the antagonist effects on MAPKs signaling and on platelet aggregation, processes mediated by PAR family members, including PAR2. Since the allosteric pocket binding 1-PPA is highly conserved in all the members of the PAR family, the evidence reported here suggests that 1-PPA could represent a promising new small molecule targeting PARs with antagonistic activity.
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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.