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leukotriene-C4 synthase activity

Definition

Target type: molecularfunction

Catalysis of the reaction: leukotriene C(4) = glutathione + leukotriene A(4). [EC:4.4.1.20, RHEA:17617]

Leukotriene-C4 synthase activity is a crucial enzymatic function involved in the biosynthesis of leukotriene C4 (LTC4), a potent inflammatory mediator. This enzyme, also known as LTC4 synthase, catalyzes the transfer of glutathione (GSH) from glutathione S-transferase to leukotriene A4 (LTA4). This reaction results in the formation of LTC4, the first member of the cysteinyl leukotriene family. The active site of LTC4 synthase exhibits a high degree of selectivity for LTA4, ensuring the specific production of LTC4. LTC4, in turn, plays a significant role in various physiological processes, including inflammation, bronchoconstriction, and immune responses. It exerts its effects by binding to specific receptors, primarily CysLT1 and CysLT2 receptors, located on various cells, such as smooth muscle cells, mast cells, and eosinophils. The activation of these receptors triggers a cascade of intracellular signaling events, leading to the release of inflammatory mediators, such as histamine, and the contraction of smooth muscle cells. Leukotriene-C4 synthase activity, therefore, is essential for the generation of a potent inflammatory mediator, LTC4, which plays a critical role in various physiological and pathological processes.'
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Proteins (2)

ProteinDefinitionTaxonomy
Arachidonate 5-lipoxygenase-activating proteinAn arachidonate 5-lipoxygenase-activating protein that is encoded in the genome of human. [PRO:DNx, UniProtKB:P20292]Homo sapiens (human)
Leukotriene C4 synthaseA leukotriene C4 synthase that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16873]Homo sapiens (human)

Compounds (12)

CompoundDefinitionClassesRoles
acetaminophenAcetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.

paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group.
acetamides;
phenols
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
cyclooxygenase 3 inhibitor;
environmental contaminant;
ferroptosis inducer;
geroprotector;
hepatotoxic agent;
human blood serum metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
acetazolamideAcetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)monocarboxylic acid amide;
sulfonamide;
thiadiazoles
anticonvulsant;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
zonisamidezonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position.

Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.
1,2-benzoxazoles;
sulfonamide
anticonvulsant;
antioxidant;
central nervous system drug;
protective agent;
T-type calcium channel blocker
zileuton1-benzothiophenes;
ureas
anti-asthmatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor;
leukotriene antagonist;
non-steroidal anti-inflammatory drug
mk 0591MK 0591: structure given in first source; MK 0591 was previously L-686,708; inhibits leukotriene biosynthesis by inhibiting 5-lipoxygenase activating protein
1-(2-chlorobenzyl)-2-(1-(4-isobutylphenyl)ethyl)-1h-benzimidazole1-(2-chlorobenzyl)-2-(1-(4-isobutylphenyl)ethyl)-1H-benzimidazole: targets 5-lipoxygenase-activating protein to inhibit leukotriene biosynthesis; structure in first source
l 6635363-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid : A member of the class of indoles that is 1H-indole substituted by a isopropyl group at position 5, a tert-butylsulfanediyl group at position 3, a 4-chlorobenzyl group at position 1 and a 2-carboxy-2-methylpropyl group at position 2. It acts as an inhibitor of arachidonate 5-lipoxygenase.

MK-886: orally active leukotriene biosynthesis inhibitor
aryl sulfide;
indoles;
monocarboxylic acid;
monochlorobenzenes
antineoplastic agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
leukotriene antagonist
montelukastmontelukast: a leukotriene D4 receptor antagonistaliphatic sulfide;
monocarboxylic acid;
quinolines
anti-arrhythmia drug;
anti-asthmatic drug;
leukotriene antagonist
psoralidinpsoralidin : A member of the class of coumestans that is coumestan substituted by hydroxy groups at positions 3 and 9 and a prenyl group at position 2 respectively.coumestans;
delta-lactone;
polyphenol
estrogen receptor agonist;
plant metabolite
topiramatetopiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine.

Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.
cyclic ketal;
ketohexose derivative;
sulfamate ester
anticonvulsant;
sodium channel blocker
bwa 4c
p-Glu-Arg-Pro-Arg-Leu-Ser-His-Lys-Gly-Pro-Met-Pro-Phep-Glu-Arg-Pro-Arg-Leu-Ser-His-Lys-Gly-Pro-Met-Pro-Phe : A thirteen-membered polypeptide consisting of p-Glu, Arg, Pro, Arg, Leu, Ser, His, Lys, Gly, Pro, Met, Pro and Phe residues joined in sequence.polypeptideapoptosis inhibitor;
human metabolite;
neuroprotective agent