Jalal Soubhye*, Pierre van Antwerpen and Francois Dufrasne Pages 2418 - 2447 ( 30 )
Group IV cytosolic phospholipase A2 (cPLA2α) plays a critical role in inflammatory processes. It produces arachidonic acid which is the main source of the pro-inflammatory eicosanoids mediators that are important in innate immune system. In some cases, these proinflammatory mediators cause damages to the host tissues and therefore promote autoimmune diseases. Consequently, development of potent inhibitors against cPLA2α could improve the therapy of inflammatory diseases. In the last two decades, intense efforts have been done to find potent cPLA2α inhibitors. Several scaffolds have been developed with the use of structureactivity relationship (SAR) studies, and potent inhibitors have been obtained. The poor absorption of these compounds from intestine was the main challenge for clinical application. This review illustrates the search for cPLA2α inhibitors, their SAR studies and biological effects.
Cytosolic phospholipase A2α, inflammation, anti-inflammatory, cPLA2α inhibitors, structure-activity relationship, arachidonic acid.
Department of Pharmacognosy, Bioanalysis and Drug Discovery, Faculty of Pharmacy, Université Libre de Bruxelles (ULB), Boulevard du Triomphe, 1050 Bruxelles, Department of Pharmacognosy, Bioanalysis and Drug Discovery, Faculty of Pharmacy, Université Libre de Bruxelles (ULB), Boulevard du Triomphe, 1050 Bruxelles, Microbiology, Bioorganic and Macromolecular Chemistry, Faculty of Pharmacy, Université Libre de Bruxelles, Campus de la Plaine, Boulevard du Triomphe, 1050 Bruxelles