Application | Comment | Organism |
---|---|---|
analysis | although structural differences near the active site and along the C-terminal alpha-helix V suggest that the mouse and human enzymes may function differently in vivo, the mouse enzyme is a useful tool in pharmacological research and drug development | Mus musculus |
drug development | although structural differences near the active site and along the C-terminal alpha-helix V suggest that the mouse and human enzymes may function differently in vivo, the mouse enzyme is a useful tool in pharmacological research and drug development | Mus musculus |
Cloned (Comment) | Organism |
---|---|
recombinant enzyme expression in Pichia pastoris strain KM71H | Mus musculus |
Crystallization (Comment) | Organism |
---|---|
purified enzyme in apoform or in complex with substrate glutathione or product analogue S-hexyl-GSH, mixing of 0.001 ml of 3.5 mg/ml protein in 0.03% w/v DDM w/v, 20 mM Tris pH 8.0, 100 mM NaCl, and 0.5 mM TCEP, with or without 1 mM GSH, with 0.001 ml of reservoir solution containing 1.8-2.2 M NH4SO4, 0.2 M NaCl and 0.1 M Na cacodylate pH 6.1-6.8, for S-hexyl GSH-enzyme crystals, S-hexyl GSH is added to mother liquor and soaking of apo-crystals, X-ray diffraction structure determination and analysis at 2.65-2.7 A resolution | Mus musculus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-benzoyl-5-(5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl)benzoic acid | i.e. TK04, competitive mode of binding versus leukotriene A4 | Mus musculus |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Michaelis-Menten kinetics | Mus musculus | |
0.036 | - |
leukotriene A4 | pH 7.8, temperature not specified in the publication, recombinant enzyme | Mus musculus | |
1.2 | - |
glutathione | pH 7.8, temperature not specified in the publication, recombinant enzyme | Mus musculus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
endoplasmic reticulum membrane | integral membrane protein in the outer leaflet of the nuclear envelope and in the endoplasmic reticulum | Mus musculus | 5789 | - |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
18000 | - |
3 * 18000 | Mus musculus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
leukotriene A4 + glutathione | Mus musculus | - |
leukotriene C4 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mus musculus | Q60860 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
leukotriene A4 + glutathione | - |
Mus musculus | leukotriene C4 | - |
? | |
leukotriene A4 + glutathione | glutathione-enzyme binding structure, overview | Mus musculus | leukotriene C4 | i.e. (5S)-hydroxy-(6R)-S-glutathionyl-7,9-trans-11,14-cis-eicosatetraenoic acid | ? | |
additional information | binding structure of product analogue S-hexyl GSH to the active site of the enzyme, overview | Mus musculus | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
trimer | 3 * 18000 | Mus musculus |
Synonyms | Comment | Organism |
---|---|---|
leukotriene C4 synthase | - |
Mus musculus |
LT C4 synthase | - |
Mus musculus |
LTC4S | - |
Mus musculus |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
81 | - |
leukotriene A4 | pH 7.8, temperature not specified in the publication, recombinant enzyme | Mus musculus | |
84 | - |
glutathione | pH 7.8, temperature not specified in the publication, recombinant enzyme | Mus musculus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.8 | - |
assay at | Mus musculus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000037 | - |
2-benzoyl-5-(5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl)benzoic acid | pH 7.8, temperature not specified in the publication, recombinant enzyme | Mus musculus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000135 | - |
pH 7.8, temperature not specified in the publication, recombinant enzyme | Mus musculus | 2-benzoyl-5-(5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl)benzoic acid |
General Information | Comment | Organism |
---|---|---|
evolution | the enzyme belongs to the superfamily of membrane-associated proteins in eicosanoid and glutathione metabolism, which consists of six integral membrane proteins. Although structural differences near the active site and along the C-terminal alpha-helix V suggest that the mouse and human enzymes may function differently in vivo | Mus musculus |
physiological function | the enzyme catalyzes the conjugation reaction between the fatty acid leukotriene A4 and GSH to form the pro-inflammatory leukotriene C4, an important mediator of asthma | Mus musculus |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
68 | - |
glutathione | pH 7.8, temperature not specified in the publication, recombinant enzyme | Mus musculus | |
2300 | - |
leukotriene A4 | pH 7.8, temperature not specified in the publication, recombinant enzyme | Mus musculus |