Phospholipases A2

Inhibition of secreted phospholipases A2 by 2-oxoamides based on $α$-amino acids: Synthesis, in vitro evaluation and molecular docking calculations

Group IIA secreted phospholipase A2 (GIIA sPLA₂) is a member of the mammalian sPLA₂ enzyme family and is associated with various inflammatory conditions. In this study, the synthesis of 2-oxoamides based on $α$-amino acids and the in vitro evaluation …

Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2

We report a series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor. Using the human group X sPLA2 crystal structure, …