Neutrophil LTA4 hydrolases and leukotriene B4 receptors: effects of leukotriene epoxides and their enzymatic products.
A selection of inhibitors of rat and human neutrophil LTA4 hydrolases have been studied in vitro using partially purified enzymes. 5(S)trans 5,6 oxido-7,9-trans-11-cis-eicosatrienoic acid (LTA3) and 5(S)trans 5,6 oxido, 7,9-trans, 11,14,17-cis-eicosapentaenoic acid (LTA5) have been shown to inhibit neutrophil LTA4 hydrolases in a time-dependent manner. The products of hydrolysis of LTA3, LTA4 and LTA5 by human and rat neutrophil LTA4 hydrolase have been shown to displace [3H] LTB4 binding to human and rat neutrophil membranes. The order of displacement of [3H] LTB4 is LTB4 = LTB3 greater than LTB5 and this correlated well with their biological potencies for enhancement of neutrophil aggregation and chemokinesis.
D000818:Animals; D001095:Arachidonic Acids / Q000378:metabolism / Q000494:pharmacology*; D002462:Cell Membrane / Q000378:metabolism; D015118:Eicosapentaenoic Acid / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D004851:Epoxide Hydrolases / Q000037:antagonists & inhibitors / Q000502:physiology*; D006801:Humans; D006868:Hydrolysis; D017572:Leukotriene A4; D007975:Leukotriene B4 / Q000378:metabolism* / Q000031:analogs & derivatives; D009504:Neutrophils / Q000201:enzymology* / Q000378:metabolism / Q000648:ultrastructure; D051381:Rats; D011971:Receptors, Immunologic / Q000502:physiology*; D018102:Receptors, Leukotriene B4; D013997:Time Factors
D001095:Arachidonic Acids; D017572:Leukotriene A4; D011971:Receptors, Immunologic; D018102:Receptors, Leukotriene B4; D007975:Leukotriene B4; C040212:leukotriene B5; C045722:leukotriene B3; D015118:Eicosapentaenoic Acid; D004851:Epoxide Hydrolases; C043134:leukotriene A4 hydrolase