Platelet-activating factor receptor (PTAFR) (PTAFR)

The Platelet-activating factor receptor (PTAFR) is a G protein-coupled receptor that mediates the biological effects of platelet-activating factor (PAF) and various structurally related oxidized phospholipids (OxPLs) [1, 2]. PAF is a potent phospholipid mediator produced by various cells, including platelets, neutrophils, and macrophages, in response to inflammatory stimuli [2]. Upon ligand binding, PTAFR activates multiple signaling pathways, including the Gq/11 and Gi/o families, leading to calcium mobilization, platelet aggregation, and the release of inflammatory cytokines [1, 3]. Oxidized phospholipids, which are generated during lipid peroxidation, can also act as agonists or modulators of PTAFR, contributing to the pathogenesis of atherosclerosis and chronic inflammatory diseases [3, 4]. Because of its central role in inflammation and allergy, PTAFR is a significant therapeutic target. Drugs such as rupatadine act as antagonists to block these pathways, providing relief in conditions like allergic rhinitis and urticaria [5]. Research into PTAFR antagonists has also explored their potential in treating acute pancreatitis, asthma, and septic shock [4, 5].

Other names

PAF receptorPAFRPlatelet-activating factor receptorPlatelet-activating factor and structurally related oxidized phospholipids

Competitive antagonism of the Platelet-activating factor receptor (PTAFR), which prevents the binding of PAF and oxidized phospholipids, thereby inhibiting pro-inflammatory signaling and platelet activation.