Page last updated: 2024-10-24

leukotriene-A4 hydrolase activity

Definition

Target type: molecularfunction

Catalysis of the reaction: H2O + leukotriene A(4) = leukotriene B(4). [EC:3.3.2.6, RHEA:22324]

Leukotriene-A4 hydrolase (LTA4H) is an enzyme responsible for the conversion of leukotriene A4 (LTA4), a highly reactive epoxide, to leukotriene B4 (LTB4). This crucial step in leukotriene biosynthesis is essential for the production of potent mediators of inflammation and immune responses. LTA4H catalyzes the nucleophilic attack of water at the epoxide group of LTA4, opening the ring and generating the alcohol group characteristic of LTB4. This enzymatic reaction occurs within the cytosol of cells, where LTA4H resides in close proximity to the enzymes responsible for the synthesis of LTA4 from arachidonic acid. LTB4, the product of this enzymatic reaction, is a potent chemoattractant and activator of neutrophils and other immune cells. It plays a critical role in the recruitment of leukocytes to sites of inflammation, the activation of inflammatory signaling pathways, and the development of inflammatory responses. The ability of LTA4H to convert LTA4 to LTB4 is thus essential for the proper functioning of the immune system and the regulation of inflammation.'
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Proteins (1)

ProteinDefinitionTaxonomy
Leukotriene A-4 hydrolaseA leukotriene A-4 hydrolase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P09960]Homo sapiens (human)

Compounds (42)

CompoundDefinitionClassesRoles
4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide4-(dimethylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)benzamide: structure in first source

4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide : A benzamide resulting from the formal condensation of the carboxy group of 4-(dimethylamino)benzoic acid with the amino group of 7-amino-N-hydroxyheptanamide. It is a potent inhibitor of histone deacetylases and induces cell cycle arrest and apoptosis in several human cancer cell lines.
benzamides;
hydroxamic acid;
secondary carboxamide;
tertiary amino compound
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
entinostatbenzamides;
carbamate ester;
primary amino compound;
pyridines;
substituted aniline
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
nimesulidenimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups.

nimesulide: structure
aromatic ether;
C-nitro compound;
sulfonamide
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
scriptaidscriptide: provokes translocation of GLUT4 to increase glucose uptake; structure in first sourceisoquinolines
vorinostatvorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).

Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.
dicarboxylic acid diamide;
hydroxamic acid
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
phenyl etherdiphenyl ether : An aromatic ether in which the oxygen is attached to two phenyl substituents. It has been found in muscat grapes and vanilla.aromatic etherplant metabolite
4-phenoxyphenolphenoxyphenol
5-hydroxyindolehydroxyindoleshuman metabolite
2-aminotetralin2-aminotetralin: RN given refers to parent cpd without isomeric designation; structuretetralins
captoprilcaptopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.

Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.
alkanethiol;
L-proline derivative;
N-acylpyrrolidine;
pyrrolidinemonocarboxylic acid
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
zileuton1-benzothiophenes;
ureas
anti-asthmatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor;
leukotriene antagonist;
non-steroidal anti-inflammatory drug
5-fluoroindolefluoroindole
beta-tetralone
ubenimexubenimex: growth inhibitor
5-chloroindole5-chloroindole: a positive allosteric modulator of the 5-HT3 receptor
5-benzyloxytryptophan
tesmilifenediarylmethane
kelatorphankelatorphan: inhibitor of enkephalin metabolism; structure given in first source
alanine-4-nitroanilidealanine-4-nitroanilide: substrate for aminopeptidase M
pyrrolidino-benzylphenoxyethanamine
dihydroresveratroldihydroresveratrol : A stilbenol that is 1,1'-ethane-1,2-diyldibenzene with hydroxy groups at positions 1, 3 and 4'.

dihydroresveratrol: structure in first source
stilbenolplant metabolite;
xenobiotic metabolite
4-(2-Amino-1,3-thiazol-4-yl)phenolphenols
trichostatin atrichostatin A: chelates zinc ion in the active site of histone deacetylases, resulting in preventing histone unpacking so DNA is less available for transcription; do not confuse with TRICHOSANTHIN which is a protein; found in STREPTOMYCESantibiotic antifungal agent;
hydroxamic acid;
trichostatin
bacterial metabolite;
EC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector
resveratroltrans-resveratrol : A resveratrol in which the double bond has E configuration.resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
leukotriene a4leukotriene A4 : A leukotriene that is the (5S,6S)-epoxy derivative of (7E,9E,11Z,14Z)-icosa-7,9,11,14-tetraenoic acid.

Leukotriene A4: (2S-(2 alpha,3 beta(1E,3E,5Z,8Z)))-3-(1,3,5,8-Tetradecatetraenyl)oxiranebutanoic acid. An unstable allylic epoxide, formed from the immediate precursor 5-HPETE via the stereospecific removal of a proton at C-10 and dehydration. Its biological actions are determined primarily by its metabolites, i.e., LEUKOTRIENE B4 and cysteinyl-leukotrienes. Alternatively, leukotriene A4 is converted into LEUKOTRIENE C4 by glutathione-S-transferase or into 5,6-di-HETE by the epoxide-hydrolase. (From Dictionary of Prostaglandins and Related Compounds, 1990)
epoxy fatty acid;
leukotriene;
long-chain fatty acid;
oxylipin;
polyunsaturated fatty acid
human metabolite;
mouse metabolite;
plant metabolite
shogaolshogaol: from ginger, ZINGIBER OFFICINALE; less mutagenic than GINGEROL; structure given in first sourceenone;
monomethoxybenzene;
phenols
tubacintubacin: inhibits histone deacetylase 6; structure in first source1,3-oxazoles
belinostathydroxamic acid;
olefinic compound;
sulfonamide
antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor
panobinostatpanobinostat : A hydroxamic acid obtained by formal condensation of the carboxy group of (2E)-3-[4-({[2-(2-methylindol-3-yl)ethyl]amino}methyl)phenyl]prop-2-enoic acid with the amino group of hydroxylamine. A histone deacetylase inhibitor used (as its lactate salt) in combination with bortezomib and dexamethasone for the treatment of multiple myeloma.

Panobinostat: An indole and hydroxamic acid derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used as an antineoplastic agent in combination with BORTEZOMIB and DEXAMETHASONE for the treatment of MULTIPLE MYELOMA.
cinnamamides;
hydroxamic acid;
methylindole;
secondary amino compound
angiogenesis modulating agent;
antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor
givinostatcarbamate ester
sc 57461SC 57461: a leukotriene A4 hydrolase inhibitor; structure given in first source
sc 57461
ala-thr-trp-leu-pro-pro-arg
mocetinostatmocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).

mocetinostat: undergoing phase II clinical trials for treatment of cancer
aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent
quisinostatindoles
resminostatresminostat: a histone deacetylase inhibitor; structure in first source
abexinostatabexinostat: structure in first sourcebenzofurans
valproate sodiumEpilim: oral sodium valproate used as antidepressive agent

sodium valproate : The sodium salt of valproic acid.

valproate : A branched-chain saturated fatty acid anion that is the conjugate base of valproic acid.
organic sodium saltgeroprotector
cudc 1017-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide: a histone deacetylase inhibitor; structure in first source
pracinostatpracinostat : A hydroxamic acid that is N-hydroxyacrylamide which is substituted at position 3 by a 2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl group (the E isomer). An orally available pan-histone deacetylase inhibitor with demonstrated activity in the treatment of advanced solid tumours.benzimidazole;
hydroxamic acid;
olefinic compound;
tertiary amino compound
antimalarial;
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
acy-1215ricolinostat: an HDAC6 inhibitor; structure in first sourcepyrimidinecarboxylic acid
rg2833RG2833: a histone deacetylase inhibitor; structure in first source