The 85-kDa cytosolic PLA2 (cPLA2) is present in most cells and tissues and its structural and functional properties have been described. Different agonists, growth factors and cytokines activate cPLA2 to hydrolyze cellular phospholipids thereby providing the precursor substrates for the biosynthesis of eicosanoids and platelet-activating factor (PAF), the well-known mediators of inflammatory and allergic reactions. Recent studies discussed here suggest that cPLA2 is a receptor-regulated enzyme involved in the inflammatory response. Therefore, inhibitors of cPLA2 may be useful as therapeutic agents in the treatment of inflammatory diseases.