1-Stearyl,2-stearoylaminodeoxy phosphatidylcholine, a potent reversible inhibitor of phospholipase A2.
1-stearyl, 2-stearoylaminodeoxy phosphatidylcholine, a structurally modified phospholipid substrate analog exhibits potent and reversible inhibition of phospholipase A2 from cobra venom (N. naja naja). The apparent KI values determined in two different assay systems employing phosphatidylcholine-surfactant mixed micelles are in reasonable agreement (40 microM and 16 microM) and indicate that the inhibitor binds to the enzyme as much as two orders of magnitude more tightly than does dipalmitoyl phosphatidylcholine. With phosphatidylethanolamine as substrate, the kinetics are more complicated as the analog also exhibits activation, presumably at a second binding site on the enzyme.
D001665:Binding Sites; D006868:Hydrolysis; D007700:Kinetics; D008823:Micelles; D017830:Octoxynol; D010713:Phosphatidylcholines / Q000378:metabolism / Q000494:pharmacology*; D010714:Phosphatidylethanolamines / Q000378:metabolism; D010740:Phospholipases / Q000037:antagonists & inhibitors*; D010741:Phospholipases A / Q000037:antagonists & inhibitors*; D054467:Phospholipases A2; D011092:Polyethylene Glycols; D011485:Protein Binding; D011663:Pulmonary Surfactants / Q000378:metabolism; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D008823:Micelles; D010713:Phosphatidylcholines; D010714:Phosphatidylethanolamines; D011663:Pulmonary Surfactants; D011092:Polyethylene Glycols; C049379:1-stearyl-2-stearoylaminodeoxyphosphatidylcholine; D017830:Octoxynol; C049380:1,2-bis(decanoylthio)-1,2-dideoxy-sn-glycerol-3-phosphorylcholine; C049381:1,2-bis(decanoylthio)-1,2-dideoxyglycerol-3-phosphorylethanolamine; D010740:Phospholipases; D010741:Phospholipases A; D054467:Phospholipases A2