GK241

GK241 (compound 31a-c) is a 2-oxoamide-based compound that has inhibitory activity against human and mouse group IIA secretory phospholipase A2 (GIIA sPLA2) (IC50 of 143 nM and 68 nM, respectively), and its inhibitory mechanism was studied by molecular dynamics simulation.

[1] Development of a potent 2-oxoamide inhibitor of secreted phospholipase A2 guided by molecular docking calculations and molecular dynamics simulations
[2] MARIA A THEODOROPOULOU. Identification of a Dual Inhibitor of Secreted Phospholipase A2 (GIIA sPLA2) and SARS-CoV-2 Main Protease.[J]. Pharmaceuticals (Basel, Switzerland), 2022. DOI: 10.3390/ph15080961
[3] SOFIA VASILAKAKI . Inhibitors of secreted phospholipase A2 suppress the release of PGE2 in renal mesangial cells[J]. Bioorganic & Medicinal Chemistry, 2016, 24 13: Pages 3029-3034. DOI: 10.1016/j.bmc.2016.05.017