3.3.2.6: leukotriene-A4 hydrolase
This is an abbreviated version!
For detailed information about leukotriene-A4 hydrolase, go to the full flat file.
Word Map on EC 3.3.2.6
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3.3.2.6
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5-lipoxygenase
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arachidonic
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epoxide
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medicine
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leukocyte
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asthma
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bestatin
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chemoattractant
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eicosanoids
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metalloenzyme
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flap
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ionophore
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alox5ap
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tuberculous
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transcellular
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5-lipoxygenase-activating
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aminopeptidases
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captopril
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lipoxins
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pro-gly-pro
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montelukast
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proline-glycine-proline
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5-hete
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zileuton
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diagnostics
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pharmacology
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drug development
- 3.3.2.6
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5-lipoxygenase
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arachidonic
- epoxide
- medicine
- leukocyte
- asthma
- bestatin
-
chemoattractant
-
eicosanoids
-
metalloenzyme
- flap
-
ionophore
-
alox5ap
-
tuberculous
-
transcellular
-
5-lipoxygenase-activating
- aminopeptidases
- captopril
-
lipoxins
- pro-gly-pro
- montelukast
- proline-glycine-proline
-
5-hete
- zileuton
- diagnostics
- pharmacology
- drug development
Reaction
Synonyms
EH, epoxide hydrolase, hydrolase, leukotriene A4, leukotriene A(4) hydrolase, leukotriene A4 hydrolase, leukotriene A4 hydrolase/aminopeptidase, leukotriene hydrolase A4, leukotriene-A4 hydrolase, leukotriene-A4-hydrolase, LT A4 hydrolase, LTA-4 hydrolase, LTA4 hydrolase, LTA4-h, LTA4H, More
ECTree
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Inhibitors
Inhibitors on EC 3.3.2.6 - leukotriene-A4 hydrolase
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(1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)-carbamic acid tert-butyl ester
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(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[(4-nitrobenzyl)sulfanyl]propanoic acid
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(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[(4-phenoxybenzyl)sulfanyl]propanoic acid
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(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[(4-propylbenzyl)sulfanyl]propanoic acid
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(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[[4-(trifluoromethoxy)benzyl]sulfanyl]propanoic acid
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(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[[4-(trifluoromethyl)benzyl]sulfanyl]propanoic acid
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(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-(1,2,4-oxadiazol-2(3H)-ylmethyl)piperidine
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(2R)-3-(benzylsulfanyl)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[(4-bromobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[(4-chlorobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[(4-cyanobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[(4-ethoxybenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[(4-ethylbenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[(4-fluorobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[(4-iodobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[(4-methoxybenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[(4-methylbenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[(biphenyl-4-ylmethyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[[3-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[[4-(1-methylethyl)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(3-sulfanylbutanoyl)amino]propanoic acid
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(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(3-sulfanylpropanoyl)amino]propanoic acid
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(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(4-sulfanylbutanoyl)amino]propanoic acid
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(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(sulfanylacetyl)amino]propanoic acid
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(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2R)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2R)-2-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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SA6541
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[[4-(methoxysulfinyl)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2R)-3-[[4-(methylsulfanyl)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2S)-1-[(2R)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
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5% inhibition at 1 mM
(2S)-2-amino-3-[4-(benzyloxy)phenyl]propane-1-thiol
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it are about 50 derivates and related structures synthesized and assayed their inhibition of enzyme catalyzes hxdrolysis of L-alanine-4-nitroanilide
(2S)-2-amino-N-[4-(phenylmethoxy)phenyl]-3-[4-(1H-imidazole)]propanamide dihydrochloride
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(2S)-2-amino-N-[4-(phenylmethoxy)phenyl]benzenepropanamide hydrochloride
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(2S)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
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(2S)-4-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]butanoic acid
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(2S)-N-[4-(phenylmethoxy)phenyl]-2-pyrrolidinecarboxamide hydrochloride
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(2S,4R)-3-(2-methyl-3-sulfanylpropanoyl)-2-naphthalen-1-yl-1,3-thiazolidine-4-carboxylic acid
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58% inhibition at 1 mM
(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(2-phenylethyl)sulfanyl]pyrrolidine-2-carboxylic acid
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(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(3-phenylpropyl)sulfanyl]pyrrolidine-2-carboxylic acid
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(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(naphthalen-1-ylmethyl)sulfanyl]pyrrolidine-2-carboxylic acid
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(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(naphthalen-2-ylmethyl)sulfanyl]pyrrolidine-2-carboxylic acid
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(2S,4S)-4-(benzylsulfanyl)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
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(2S,4S)-4-[(2-methylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
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(2S,4S)-4-[(3-methylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
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(2S,4S)-4-[[4-(methylsulfanyl)benzyl]sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
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(4R)-2-furan-2-yl-3-[(2S)-2-methyl-3-sulfanylpropanoyl]-1,3-thiazolidine-4-carboxylic acid
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36% inhibition at 1 mM
(4R)-3-[(2R)-2-methyl-3-sulfanylpropanoyl]-1,3-thiazolidine-4-carboxylic acid
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18% inhibition at 1 mM
(4R)-3-[(2S)-2-methyl-3-sulfanylpropanoyl]-1,3-thiazolidine-4-carboxylic acid
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58% inhibition at 1 mM
(4R)-3-[(2S)-2-methyl-3-sulfanylpropanoyl]-2-pyridin-4-yl-1,3-thiazolidine-4-carboxylic acid
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25% inhibition at 1 mM
(4R)-3-[(2S)-2-methyl-3-sulfanylpropanoyl]-2-thiophen-2-yl-1,3-thiazolidine-4-carboxylic acid
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14% inhibition at 1 mM
(4R)-4-[[4-(1-methylethyl)benzyl]sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
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(4S)-4-([2-[4-(1-methylethyl)phenyl]ethyl]sulfanyl)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
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(4S)-4-([3-[4-(1-methylethyl)phenyl]propyl]sulfanyl)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
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(4S)-4-amino-4-(2-(1,3,4-triazolyl))-N-(4-phenoxyphenyl)butanamide trifluoroacetate
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(4S)-4-amino-5-(1-phthalimido)-N-(4-phenoxyphenyl)pentanamide trifluoroacetate
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(4S)-4-amino-5-(1H-pyrrol-1-yl)-N-(4-phenoxyphenyl)pentanamide bistrifluoroacetate
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(4S)-4-amino-5-(2-thio-5-amino-1,3,4-thiadiazol-2-yl)-N-(4-phenoxyphenyl)pentanamide bistrifluoroacetate
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(4S)-4-[(4-cyclohexylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
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(4S)-4-[(4-tert-butylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
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(4S)-4-[[4-(1-methylethyl)benzyl]sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
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(R)-5-(1,2-dithiolan-3-yl) pentanoic acid
i.e. alpha-lipoic acid, inhibits both activities of the enzyme at concentrations lower than 0.010 mM. The carboxylate group of alpha lipoic acid situates at 3 A from important residues R563 and K565 in the catalytic pocket of the protein, suggesting that alpha lipoic acid participates in electrostatic interactions with these residues
(S)-2-((S)-2-(2-(((R)-1-amino-2-phenylethyl)(hydroxy)phosphoryl)acetamido)-3-phenylpropanamido)-3-phenylpropanoic acid
RB3041, tight slow-binding LTA4H inhibitor
(S)-2-((S)-2-(2-(((R)-1-aminoethyl)(hydroxy)phosphoryl)acetamido)-3-(biphenyl-4-yl)propanamido)propanoic acid
RB3040, tight slow-binding LTA4H inhibitor
1-(1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
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1-(1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-yl)pyrrolidin-2-one
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1-(1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
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1-(1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]piperidin-4-yl)pyrrolidin-2-one
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1-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
1-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
1-(2-(4-(2-(trifluoromethyl)phenoxy)phenoxy)ethyl)pyrrolidine
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dual target inhibitor against cyclooxygenase COX-2 and leukotriene A4 hydrolyase in the enzyme assays and the human whole blood assay with IC50 values in the micromolar to submicromolar range. Inhibitor shows good selectivity for COX-2 over COX-1
1-(2-(4-(2-nitrophenoxy)phenoxy)ethyl)pyrrolidine
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dual target inhibitor against cyclooxygenase COX-2 and leukotriene A4 hydrolyase in the enzyme assays and the human whole blood assay with IC50 values in the micromolar to submicromolar range. Inhibitor shows good selectivity for COX-2 over COX-1
1-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-2-[[4-(furan-2-yl)-5-hydroxy-4H-1,2,4-triazol-3-yl]sulfanyl]ethanone
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compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
1-(5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
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1-(5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
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1-(5-[[5-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[5-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[5-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-([4-[(1,3-benzothiazol-2-yl)oxy]phenyl]methyl)piperidine-4-carboxylic acid
i.e. JNJ-26993135
1-[1-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]piperidin-4-yl]pyrrolidin-2-one
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1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidine-4-carboxylic acid amide
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1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidine-4-carboxylic acid amide
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1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]piperidine-4-carboxamide
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1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]piperidine-4-carboxamide
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1-[5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]ethanone
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1-[5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]ethanone
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1-[5-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]-2,5-diazabicyclo[2.2.1]hept-2-yl]ethanone
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1-[5-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]ethanone
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1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
2,3-Butanedione
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preincubation with bestatin partially protects enzyme from inactivation
2,4-dimethyl-N-[[2-(thiophen-2-yl)-1,3-thiazol-4-yl]methyl]-1,3-thiazole-5-sulfonamide
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compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
2-bromo-4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
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2-fluoro-4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
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2-[4-(2-morpholin-4-ylethoxy)phenoxy]-1-(2-trimethylsilanylethoxymethyl)-1H-benzoimidazole
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2-[[4-methyl-5-([[2-oxo-2-(phenylamino)ethyl]sulfanyl]methyl)-4H-1,2,4-triazol-3-yl]sulfanyl]-N-phenylacetamide
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compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
3-(1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)oxazolidin-2-one
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3-(1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-yl)oxazolidin-2-one
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3-(4-fluorophenyl)-5-[2-methyl-5-(pyrrolidin-1-ylsulfonyl)furan-3-yl]-1,2,4-oxadiazole
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compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
3-fluoro-4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
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3-[[4-(1-methylethyl)benzyl]sulfanyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-valine
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4'-O-methyl shogoal
a potent enzyme inhibitor, non-cytotoxic to normal cells
4-((R)-2-(4-(4-chlorophenoxy)phenoxymethyl)pyrrolidin-1-yl)-l-butyric acid
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4-((S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl)-butyric acid
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4-([(1R,5S)-3-[(4-benzylphenyl)amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl)benzoic acid
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4-([(1R,5S)-3-[(4-phenoxyphenyl)amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl)benzoic acid
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4-([(2R)-2-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]pyrrolidin-1-yl]methyl)benzoic acid
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4-([2-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]pyrrolidin-1-yl]methyl)benzoic acid
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4-([4-[([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)methyl]piperidin-1-yl]methyl)benzoic acid
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4-([methyl[2-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)ethyl]amino]methyl)benzoic acid
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4-([methyl[2-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)ethyl]amino]methyl)benzoic acid
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4-([methyl[3-([2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl]amino]methyl)benzoic acid
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4-([methyl[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)propyl]amino]methyl)benzoic acid
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4-([methyl[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)cyclohexyl]amino]methyl)benzoic acid
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4-([[2,2-dimethyl-3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl](methyl)amino]methyl)benzoic acid
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4-([[3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl]amino]methyl)benzoic acid
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4-([[3-([2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl]amino]methyl)benzoic acid
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4-([[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)cyclohexyl]amino]methyl)benzoic acid
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4-dimethylamino-N-[4-(phenylmethoxy)phenyl]-butanamide trifluoroacetate
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4-[(2S)-2-([4-(4-chlorophenoxy)phenoxy]methyl)-1-pyrrolidinyl]butanoic acid
i.e. DG-051
4-[(2S)-2-([4-[4-(thiophen-3-yl)benzyl]phenoxy]methyl)piperidin-1-yl]butanoic acid
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4-[(4-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]-1,4-diazepan-1-yl)methyl]benzoic acid
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4-[(4-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperazin-1-yl)methyl]benzoic acid
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4-[(5-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)methyl]benzoic acid
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4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]-3-nitrobenzoic acid
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4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]cyclohexanecarboxylic acid
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4-[(methyl[[(2R)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperidin-2-yl]methyl]amino)methyl]benzoic acid
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4-[(methyl[[(2R)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]pyrrolidin-2-yl]methyl]amino)methyl]benzoic acid
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4-[(methyl[[(2S)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperidin-2-yl]methyl]amino)methyl]benzoic acid
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4-[(methyl[[(2S)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]pyrrolidin-2-yl]methyl]amino)methyl]benzoic acid
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4-[2-[(1R,5S)-3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]ethyl]benzoic acid
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4-[2-[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]ethyl]benzoic acid
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4-[2-[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]ethyl]benzoic acid
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4-[[(1R,5S)-3-([4-[3-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
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JNJ-26993135
4-[[(1R,5S)-3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-([4-[4-(1,3-thiazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-([4-[4-(1H-pyrrol-1-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-([4-[4-(trifluoromethyl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(1,3-benzothiazol-2-yloxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(2-chlorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(2-fluorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(4-chlorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(4-fluorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(4-methoxyphenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(benzyloxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(biphenyl-4-yloxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(pyridin-4-ylmethyl)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(3-[[2-([4-[(2R)-2-hydroxy-2-phenylethoxy]phenyl]amino)-2-oxoethyl](methyl)amino]propyl)(methyl)amino]methyl]benzoic acid
-
-
4-[[(3R)-3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)pyrrolidin-1-yl]methyl]benzoic acid
-
-
4-[[(3S)-3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)pyrrolidin-1-yl]methyl]benzoic acid
-
-
4-[[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]methyl]benzoic acid
-
-
4-[[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)pyrrolidin-1-yl]methyl]benzoic acid
-
-
4-[[4-(1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]hydrazino)piperidin-1-yl]methyl]benzoic acid
-
-
4-[[4-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)azepan-1-yl]methyl]benzoic acid
-
-
4-[[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)azepan-1-yl]methyl]benzoic acid
-
-
4-[[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]methyl]benzoic acid
-
-
4-[[methyl(1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]azepan-4-yl)amino]methyl]benzoic acid
-
-
4-[[methyl(1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperidin-4-yl)amino]methyl]benzoic acid
-
-
4-[[methyl(3-[methyl[2-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-2-oxoethyl]amino]propyl)amino]methyl]benzoic acid
-
-
4-[[[3-[(2-[[4-(2-fluorophenoxy)phenyl]amino]-2-oxoethyl)(methyl)amino]propyl](methyl)amino]methyl]benzoic acid
-
-
4-[[[3-[(2-[[4-(4-chlorophenoxy)phenyl]amino]-2-oxoethyl)(methyl)amino]propyl](methyl)amino]methyl]benzoic acid
-
-
4-[[[3-[(2-[[4-(4-fluorophenoxy)phenyl]amino]-2-oxoethyl)(methyl)amino]propyl](methyl)amino]methyl]benzoic acid
-
-
4-[[[3-[[2-[(4-benzylphenyl)amino]-2-oxoethyl](methyl)amino]propyl](methyl)amino]methyl]benzoic acid
-
-
5-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]furan-2-carboxylic acid
-
-
acetic acid (1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-ylcarbamoyl)methyl ester
-
-
acetic acid [1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-ylcarbamoyl]methyl ester
-
-
Acetic anhydride
-
complete loss of peptidase activity and epoxide hydrolase activity
acrolein
acrolein in cigarette smoke in part inhibits LTA4H peptidase activity
citraconic anhydride
-
complete loss of peptidase activity and epoxide hydrolase activity
diamide/glutathione combination
-
complete loss of peptidase activity and epoxide hydrolase activity
-
JNJ 26993135
-
a selective LTA4H inhibitor, leads to reduction of TH2 cytokines and mucin levels, and blocks mast cell production of LTB4 and suppresses airway hyperresponsiveness
JNJ-26993135
shows selective inhibition of LTB4 biosynthesis in a murine model, suggesting a potent compound targeting LTA4H
leukotriene A4 ethyl ester
-
comparison of inactivation of wild-type and mutant enzymes
methyl 5-(1,2-dithiolan-3-yl) pentanoate
i.e. alpha-lipoic acid methyl ester or LAME
methyl methanethiosulfonate
-
inhibition of epoxide hydrolase activity, stimulation of peptidase activity
methyl-methane thiosulfonate
-
inhibits aminopeptidase activity and NaCl stimulates this inactivation, beta-mercaptoethanol reactivates this inactivation, bestatin protects inactivation, little effect on epoxid hydrolase activity
N-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
N-(2-[[6-(4-fluorophenyl)pyridazin-3-yl]amino]ethyl)-1,2-dimethyl-1H-imidazole-4-sulfonamide
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
N-(8-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]-8-azabicyclo[3.2.1]oct-3-yl)acetamide
-
-
N-(8-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]-8-azabicyclo[3.2.1]oct-3-yl)acetamide
-
-
N-Acetylimidazole
-
75 min, loss of 92% peptidase activity and 78% of epoxide hydrolase activity, both activities are restored by hydroxylamine and bestatin protects
N-[(3-endo)-8-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
N-[(3-endo)-8-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
N-[2-[(furan-2-ylmethyl)sulfanyl]ethyl]-2-[[1-(4-hydroxyphenyl)-1H-tetrazol-5-yl]sulfanyl]acetamide
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
N-[3(R)-[(hydroxyamino)carbonyl]-2-benzyl-1-oxopropyl]-L-alanine
i.e. kelatorphan, potent inhibitor of Zn-metalloenzymes
N-[3-[3-(acetylamino)phenoxy]propyl]-3-[3-(pyridin-2-yl)-1,2,4-oxadiazol-5-yl]propanamide
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
N-[4-(3-chlorophenyl)-2,5-dioxopiperazin-1-yl]-2-[[4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]acetamide
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
N-[8-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
-
N1-(2-carboxyethyl)-N5-(4-phenoxyphenyl)-L-glutamamide trifluoroacetate
-
N1-(2-hydroxyethyl)-N5-(4-phenoxyphenyl)-L-glutamamide trifluoroacetate
-
N1-(3-carboxypropyl)-N5-(4-phenoxyphenyl)-L-glutamamide trifluoroacetate
-
N1-(4-carboxybutyl)-N5-(4-phenoxyphenyl)-L-glutamamide bistrifluoroacetate
-
N2-methyl-N2-[3-[methyl(4-oxobutyl)amino]propyl]-N-(4-phenoxyphenyl)glycinamide
-
-
N2-methyl-N2-[4-[methyl(4-oxobutyl)amino]butyl]-N-(4-phenoxyphenyl)glycinamide
-
-
N5-[4-(N-methyl-N-phenylamino)phenyl]-L-glutamine methyl ester trifluoroacetate
-
N5-[4-[4-(1H-pyrrol-1-yl)phenoxy]phenyl]-L-glutamine hemitrifluoroacetate
-
S-(4-cyclohexylbenzyl)-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[(4-cyclohexylphenyl)(phenyl)methyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-(4-cyclohexylphenyl)-1-methylethyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-methyl-1-[4-(1-methylethyl)phenyl]ethyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-[4-(1-methylethyl)phenyl]butyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-[4-(1-methylethyl)phenyl]ethyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-[4-(1-methylethyl)phenyl]pentyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-[4-(1-methylethyl)phenyl]propyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[2-methyl-1-[4-(1-methylethyl)phenyl]propyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[4-(dimethylamino)benzyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
i.e. SA6541, a specific inhibiter of LTA4 hydrolase, that attenuates 5-lipoxygenase metabolite-induced scratching behavior, but does not affect the increase in vascular permeability caused by 5-hydroperoxyeicosatetraenoic acid, 5-HPETE, overview
S-[[4-(1-methylethyl)phenyl](phenyl)methyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
sulindac sulfide
reduces LTA4H activity in HT29 CRC cells, thus lowering LTB4 levels and decreasing HT29 cell viability
Trinitrobenzenesulfonate
-
complete loss of peptidase activity and epoxide hydrolase activity
-
(S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid
-
-
-
1-(1-[2-[4-(1,3-benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
-
-
-
-
1-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(5-[[5-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
-
JNJ-27265732
-
-
1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
-
-
-
-
1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
-
-
2-oxo-3-amino carboxylic esters
-
contain a transition state mimic of the enzyme-catalyzed amide cleavage as a core and additional complementary components which resemble the hydrophobic nature of the conjugated polyene system of the natural substrate LTA4
-
2-oxo-3-amino carboxylic esters
-
comparison of inhibition of mutant and wild-type enzymes
-
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
-
-
2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
-
-
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
enzyme binding structure, overview
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
markedly diminishes early neutrophilic inflammation in mouse models of ALI and IPF under a clinical safety dose, enzyme binding structure, overview
-
i.e. DG-051, a phase II clinical candidate
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051, a phase II clinical candidate
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
i.e. DG-051
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
i.e. DG051
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051, a phase II clinical candidate
-
i.e. DG-051 M1-A, a derivative derived from DG-051
4-[(2S)-2-[[4-(4-chloro-2-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M1-A, a derivative derived from DG-051
4-[(2S)-2-[[4-(4-chloro-2-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M1-A, a derivative derived from DG-051
-
i.e. DG-051 M1-B, a derivative derived from DG-051
4-[(2S)-2-[[4-(4-chloro-3-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M1-B, a derivative derived from DG-051
4-[(2S)-2-[[4-(4-chloro-3-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M1-B, a derivative derived from DG-051
-
i.e. DG-051 M2, an N-oxide derivative derived from DG-051
4-[(2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-oxidopyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M2, an N-oxide derivative derived from DG-051
4-[(2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-oxidopyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M2, an N-oxide derivative derived from DG-051
bestatin
isolated from Streptomyces olivoreticuli, a general AP inhibitor, inhibits LTB4 biosynthesis. Treatment with bestatin inhibits cell proliferation of lung carcinoma A549 cells by significantly reducing LTA4H activity
bestatin
significantly inhibits LTB4 production, samples from13 CRC patients show a significant decrease in LTB4, the LTA4H signaling pathway, and Ki-67 in the bestatin-treated group compared with the untreated group
bestatin
significantly inhibit LTB4 production, bestatin effectively inhibits LTB4 synthesis and tumorigenesis in the ApcMin/+ and CRC patient-derived xenograft mouse model
bestatin
bestatin inhibits leukotriene B4 biosynthesis in the esophageal tissues
bestatin
isolated from Streptomyces olivoreticuli, a general AP inhibitor, inhibits LTB4 biosynthesis. Following a short-term intraperitoneal treatment with 10 mg/kg bestatin, LTB4 biosynthesis in the esophagoduodenal junction is significantly suppressed in rats treated with EGDA compared to that in the untreated group, in an esophagogastroduodenal anastomosis (EGDA) surgical model. Bestatin inhibits LTA4H/LTB4 activation and reduces tumorigenesis in EGDA rats
bestatin
-
aminopeptidase activity, leukotriene A4 competes partially
DG-051
-
a LTA4H inhibitor, used for therapeutic modulation of the leukotriene synthesis pathway in case of myocardial infarction
leukotriene A4
-
suicide inactivation via an apparently mechanism-based irreversible binding of leukotriene A4 to the protein in a 1:1 stoichiometry, comparison of inactivation of wild-type and mutant enzymes, Tyr378 is a residue, which is involved in the binding of leukotriene A4
leukotriene A4
-
comparison of inactivation of wild-type and mutant enzymes; suicide inactivation
leukotriene A4
-
leukotriene A4 binds covalently to Tyr378 and blocks epoxide hydrolase and aminopeptidase activities
leukotriene A4
-
pre-treatment of enzyme by methyl-methane thiosulfonate does not protect against suicide inactivation by leukotriene A4
leukotriene A4
-
inhibits epoxid hydrolase activity and stimulates peptidase activity
leukotriene A4 methyl ester
-
comparison of inactivation of wild-type and mutant enzymes
-
-
N-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
-
-
-
-
N-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
-
-
N-[(3-endo)-8-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
-
N-[(3-endo)-8-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
-
N-[(3-endo)-8-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
-
N-[(3-endo)-8-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
-
-
SC-57461A
resveratrol
binds directly to LTA4H and inhibits its activity. The antiproliferative effect of resveratrol is decreased in LTA4H mRNA knockdown cells, LTA4H is a direct target of resveratrol
suberanilohydroxamic acid
markedly diminishes early neutrophilic inflammation in mouse models of ALI and IPF under a clinical safety dose, enzyme binding structure, overview
-
from ginger, [6]-gingerol suppresses anchorage-independent cancer cell growth by inhibiting LTA4H activity in HCT116 colorectal cancer cells, overview. [6]-Gingerol specifically binds with LTA4H in vitro and ex vivo
[6]-gingerol
-
from ginger, [6]-gingerol suppresses anchorage-independent cancer cell growth by inhibiting LTA4H activity in mice, overview. [6]-Gingerol specifically binds with LTA4H in vitro and ex vivo
additional information
-
some enzyme inhibitors also affect the cytotoxicity of the anthrax lethal factor on macrophage cell lines
-
additional information
-
leukotriene A4 inhibitors based on piperidine and piperazine scaffolds, overview
-
additional information
structure-based drug discovery, inhibitor binding and molecular docking, overview
-
additional information
-
combined molecular docking and pharmacophore filtering assay for identification of chemical compounds that can simultaneously inhibit the human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S enzymes
-
additional information
-
not inhibited by NI101, 2-(5-(benzyloxy)-1H-indol-3-yl)ethanaminium chloride, 2-(5-(naphthalen-2-ylmethoxy)-1H-indol-3-yl)ethanaminiumchloride, 2-(5-(naphthalen-1-ylmethoxy)-1H-indol-3-yl)ethanaminium chloride, 2-(5-(3-phenoxybenzyloxy)-1H-indol-3-yl)ethanaminium chloride, 2-(5-(2-(4-(4-nitrophenoxy)phenoxy)ethoxy)-1H-indol-3-yl)ethanaminium chloride, 2-(5-(2-(4-(2-nitrophenoxy)phenoxy)ethoxy)-1H-indol-3-yl) ethanaminium chloride, 3-(2-(5-(3-phenoxybenzyloxy)-1H-indol-3-yl)ethylamino)propanoic acid, and 3-(2-(5-(2-(4-phenoxyphenoxy)ethoxy)-1H-indol-3-yl) ethylamino)propanoic acid
-
additional information
tosedostat, or CHR-2797 shows inhibition of the aminopeptidase activity. [6]-Gingerol and derivatives show chemopreventive effects and selective cytotoxicity toward HCT-116 cells but not toward healthy cells
-
additional information
thermodynamic properties of structurally distinct leukotriene A4 hydrolase inhibitors. An in silico method for the determination of stabilized water molecules in the binding site of the apo structure of LTA4H is used to interpret the measured thermodynamic data and provided insights for design of novel LTA4H inhibitors. Fluorescence-based assay system with recombinant His6-tagged enzyme is used for determination of the inhibition kinetics
-
additional information
synthesis, docking, cytotoxicity, and LTA4H inhibitory activity of gingerol derivatives as potential colorectal cancer therapy. NMR spectroscopic structure analysis, enzyme-inhibitor interactions, molecular modeling and docking study, overview. IC50 for cytotoxicity with HCT-116, TIG-1, and HF-1 cells
-
additional information
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synthesis, docking, cytotoxicity, and LTA4H inhibitory activity of gingerol derivatives as potential colorectal cancer therapy. NMR spectroscopic structure analysis, enzyme-inhibitor interactions, molecular modeling and docking study, overview. IC50 for cytotoxicity with HCT-116, TIG-1, and HF-1 cells
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5-lipoxygenase inhibitor zileuton, or the 5-lipoxygenase activating protein inhibitor MK-886, are unable to inhibit the activity of the enzyme. Inhibitor docking and molecular dynamics simulations, interaction analysis
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drug repurposing of histone deacetylase (HDAC) inhibitors that alleviate neutrophilic inflammation in acute lung injury and idiopathic pulmonary fibrosis via inhibiting leukotriene A4 hydrolase and blocking LTB4 biosynthesis, overview. Analysis of potential inhibitors of LTA4H across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray crystallographic investigation. Detailed mechanisms of down-regulation of proinflammatory cytokines by SAHA or M344 are determined in vivo. Cotreatment of N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide and (S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid synergistically represses the migration of neutrophil and LTB4-induced neutrophil migration is not affected by these treatments. Molecular modelling of HDAC inhibitors against LTA4H hydrolase and aminopeptidase
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additional information
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drug repurposing of histone deacetylase (HDAC) inhibitors that alleviate neutrophilic inflammation in acute lung injury and idiopathic pulmonary fibrosis via inhibiting leukotriene A4 hydrolase and blocking LTB4 biosynthesis, overview. Analysis of potential inhibitors of LTA4H across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray crystallographic investigation. Detailed mechanisms of down-regulation of proinflammatory cytokines by SAHA or M344 are determined in vivo. Cotreatment of N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide and (S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid synergistically represses the migration of neutrophil and LTB4-induced neutrophil migration is not affected by these treatments. Molecular modelling of HDAC inhibitors against LTA4H hydrolase and aminopeptidase
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additional information
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cigarette smoke exposure acidifies the airspaces and induced localization of the LTA4H protein into the nuclei of the epithelial cells. This results in accumulation of proline-glycine-proline in the airspaces by suppressing the LTA4H aminopeptidase activity
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treatment with bestatin does not inhibit cell proliferation of NIH/3T3 normal mouse embryo fibroblast cells
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additional information
drug repurposing of histone deacetylase (HDAC) inhibitors that alleviate neutrophilic inflammation in acute lung injury and idiopathic pulmonary fibrosis via inhibiting leukotriene A4 hydrolase and blocking LTB4 biosynthesis, overview. Analysis of potential inhibitors of LTA4H across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray crystallographic investigation. Detailed mechanisms of down-regulation of proinflammatory cytokines by SAHA or M344 are determined in vivo. Cotreatment of N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide and (S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid synergistically represses the migration of neutrophil and LTB4-induced neutrophil migration is not affected by these treatments. Molecular modeling of HDAC inhibitors against LTA4H hydrolase and aminopeptidase
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additional information
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drug repurposing of histone deacetylase (HDAC) inhibitors that alleviate neutrophilic inflammation in acute lung injury and idiopathic pulmonary fibrosis via inhibiting leukotriene A4 hydrolase and blocking LTB4 biosynthesis, overview. Analysis of potential inhibitors of LTA4H across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray crystallographic investigation. Detailed mechanisms of down-regulation of proinflammatory cytokines by SAHA or M344 are determined in vivo. Cotreatment of N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide and (S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid synergistically represses the migration of neutrophil and LTB4-induced neutrophil migration is not affected by these treatments. Molecular modeling of HDAC inhibitors against LTA4H hydrolase and aminopeptidase
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