scholarly journals A leukotriene C4 synthase inhibitor with the backbone of 5-(5-methylene-4-oxo-4,5-dihydrothiazol-2-ylamino) isophthalic acid

2013 ◽  
Vol 153 (5) ◽  
pp. 421-429 ◽  
Author(s):  
Hideo Ago ◽  
Noriaki Okimoto ◽  
Yoshihide Kanaoka ◽  
Gentaro Morimoto ◽  
Yoko Ukita ◽  
...  
Keyword(s):  
Isophthalic Acid ◽  
Leukotriene C4 ◽  
Synthase Inhibitor ◽  
Leukotriene C4 Synthase

scholarly journals 14,15-Dehydroleukotriene A4: a specific substrate for leukotriene C4 synthase

1997 ◽  
Vol 328 (1) ◽  
pp. 225-229 ◽  
Author(s):  
Angelo SALA ◽  
Mylene GARCIA ◽  
Simona ZARINI ◽  
Jean Claude ROSSI ◽  
Giancarlo FOLCO ◽  
...  
Keyword(s):  
Human Platelet ◽  
Leukotriene B4 ◽  
Reversed Phase ◽  
Human Platelets ◽  
Polymorphonuclear Leucocyte ◽  
Specific Substrate ◽  
Leukotriene C4 ◽  
Synthase Inhibitor ◽  
Leukotriene A4 ◽  
Leukotriene C4 Synthase

We studied the metabolism of 14,15-dehydro-leukotriene A4 (14,15-dehydro-LTA4) by human platelet leukotriene C4 (LTC4) synthase and polymorphonuclear leucocyte (PMNL) leukotriene A4 (LTA4) hydrolase. Metabolites were separated and identified using reversed-phase HPLC coupled to diode-array UV detection. Human platelets metabolize 14,15-dehydro-LTA4 to 14,15-dehydro-LTC4 with apparent kinetics identical with authentic LTA4. Metabolism to 14,15-dehydro-LTC4 is inhibited by MK-886, a reported LTC4 synthase inhibitor in human platelets, with a potency comparable with that shown by LTA4. In contrast, neither human red-blood-cell lysates nor human PMNL enzymically convert 14,15-dehydro-LTA4 into 14,15-dehydro-leukotriene B4. Minor amounts of 14,15-dehydro-LTC4, observed in some PMNL preparations, result from variable eosinophil contamination, as confirmed using highly purified neutrophil and eosinophil-enriched preparations. In addition, 14,15-dehydro-LTA4 irreversibly inhibits PMNL LTA4 hydrolase with an IC50 of 0.73 μM. The geometry of the methyl terminus of LTA4 does not influence the metabolism by human platelet LTC4 synthase. The double bond at C-14,15 is essential for the catalytic activity of LTA4 hydrolase but not for binding to this enzyme.

Leukotriene C4 Synthase: Upcoming Drug Target For Inflammation

2012 ◽  
Vol 13 (8) ◽  
pp. 1114-1125 ◽  
Author(s):  
Nisha S. Devi ◽  
Mukesh Doble
Keyword(s):  
Drug Target ◽  
Leukotriene C4 ◽  
Leukotriene C4 Synthase

scholarly journals Leukotriene C4 synthase polymorphisms and responsiveness to leukotriene antagonists in asthma

2003 ◽  
Vol 56 (4) ◽  
pp. 422-426 ◽  
Author(s):  
Graeme P. Currie ◽  
John J. Lima ◽  
Jim E. Sylvester ◽  
Daniel K. C. Lee ◽  
Wendy J. R. Cockburn ◽  
...  
Keyword(s):  
Leukotriene C4 ◽  
Leukotriene Antagonists ◽  
Leukotriene C4 Synthase

Enhanced leukotriene C4 synthase activity in thioglycollate-elicited peritoneal macrophages

1990 ◽  
Vol 171 (3) ◽  
pp. 1344-1352 ◽  
Author(s):  
Masayoshi Abe ◽  
Naohiko Hara ◽  
Hisakazu Muranishi ◽  
Tougo Ikeda ◽  
Nobuhiko Nagata ◽  
...  
Keyword(s):  
Peritoneal Macrophages ◽  
Leukotriene C4 ◽  
Leukotriene C4 Synthase
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