1-Piperidine Propionic Acid as an Allosteric Inhibitor of Protease Activated Receptor-2.

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 simulatio

SUBMITTER: Chinellato M 

PROVIDER: S-EPMC10610151 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature