par Soubhye, Jalal 
;Van Antwerpen, Pierre ;Dufrasne, François
Référence Current medicinal chemistry
Publication Publié, 2018-01
;Van Antwerpen, Pierre ;Dufrasne, François Référence Current medicinal chemistry
Publication Publié, 2018-01
Article révisé par les pairs
| Résumé : | 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 pro-inflammatory 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 structure-activity 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. |
