68729-05-5

Leukotriene A₄ (LTA₄) hydrolase/aminopeptidase is a bifunctional zinc metalloenzyme that both catalyzes the synthesis of LTB₄ from LTA₄ and cleaves the chemotactic peptide Pro-Gly-Pro. ARM1 is a thiazolamine that inhibits LTB₄ synthesis in human neutrophils (IC₅₀ = ~0.5 μM) and conversion of LTA₄ to LTB₄ by purified LTA₄ hydrolase (K_i = 2.3 μM). ARM1 does not significantly affect the hydrolysis of Pro-Gly-Pro by LTA₄ hydrolase.

Leukotriene A4 (LTA4) hydrolase/aminopeptidase is a bifunctional zinc metalloenzyme that both catalyzes the synthesis of LTB4 from LTA4 and cleaves the chemotactic peptide Pro-Gly-Pro. ARM1 is a thiazolamine that inhibits LTB4 synthesis in human neutrophils (IC50 = ~0.5 μM) and conversion of LTA4 to LTB4 by purified LTA4 hydrolase (Ki = 2.3 μM). ARM1 does not significantly affect the hydrolysis of Pro-Gly-Pro by LTA4 hydrolase.[Cayman Chemical]

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[1]. stsiapanava a, olsson u, wan m, et al. binding of pro-gly-pro at the active site of leukotriene a4 hydrolase/aminopeptidase and development of an epoxide hydrolase selective inhibitor. proc natl acad sci u s a. 2014 mar 18;111(11):4227-32.
[2]. haeggstrm jz. leukotriene a4 hydrolase/aminopeptidase, the gatekeeper of chemotactic leukotriene b4 biosynthesis. j biol chem. 2004 dec 3;279(49):50639-42.
[3]. snelgrove rj, jackson pl, hardison mt, et al. a critical role for lta4h in limiting chronic pulmonary neutrophilic inflammation. science. 2010 oct 1;330(6000):90-4.