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.
Keywords: Cytosolic phospholipase A2α, inflammation, anti-inflammatory, cPLA2α inhibitors, structure-activity
relationship, arachidonic acid.
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