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4.4.1.20: leukotriene-C4 synthase

This is an abbreviated version!
For detailed information about leukotriene-C4 synthase, go to the full flat file.

Word Map on EC 4.4.1.20

Reaction

leukotriene C4
=
leukotriene A4
 +
glutathione

Synonyms

(7E,9E,11Z,14Z)-(5S,6S)-5,6-epoxyicosa-7,9,11,14-tetraenoate:glutathione leukotriene-transferase (epoxide-ring-opening), EC 2.5.1.37, leukotriene A4:glutathione S-leukotrienyltransferase, leukotriene C4 synthase, leukotriene C4 synthetase, LT C4 synthase, LTC4 synthase, LTC4 synthetase, LTC4S, LTCS, synthase, leukotriene C4

ECTree

     4 Lyases
         4.4 Carbon-sulfur lyases
             4.4.1 Carbon-sulfur lyases (only sub-subclass identified to date)
                4.4.1.20 leukotriene-C4 synthase

Inhibitors

Inhibitors on EC 4.4.1.20 - leukotriene-C4 synthase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-benzoyl-5-(5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl)benzoic acid
i.e. TK04, competitive mode of binding versus leukotriene A4
2-benzoyl-5-[5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl]benzoic acid
potent and selective inhibitor, potently inhibits cysteinyl leukotriene biosynthesis in immune cells
2-methyl-5-(1-methylethyl)cyclohexa-2,5-diene-1,4-dione
-
5-[5-[(4-chlorophenyl)(cyclopropylmethyl)amino]pyridine-2-carbonyl]-2-(4-methoxybenzoyl)benzoic acid
compound at 6 mg/kg body weight reduces LTE4 levels in peritoneal lavage fluid by 88%and significantly decreases vascular permeability in vivo. Potent and selective inhibitor, potently inhibits cysteinyl leukotriene biosynthesis in immune cells
5-[5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl]-2-(4-methoxybenzoyl)benzoic acid
aspirin
blocks the STAT6-dependent interleukin-4-inducible expression of LTC4S
bovine serum albumin
-
5 mg, 45% inhibition
-
cysteinyl-leukotriene
-
diethylcarbamazine
-
IC50: 0.05 mM
estrone-3-sulfate
-
IC50: 1.9 mM
hexylglutathione
indomethacin
KCl
-
0.5 mM, about 25% inhibition
L-699,333
-
i.e. 2,[2-[1-(4-chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-4,5-dihydro-1H-thiopyrano[2,3,4-c,d]indol-2-yl]ethoxy]butanoic acid, reversible, competitive against glutathione and non-competitive against leukotriene A4
leukotriene A4
-
substrate inhibition
leukotriene C2
-
IC50: 0.0011 mM
leukotriene C4
leukotriene D4
-
-
leukotriene E4
-
-
MK-886
N-ethylmaleimide
inhibits the recombinant enzyme
NaCl
-
0.5 mM, about 25% inhibition
p-aminohippuric acid
-
IC50: 0.26 mM
probenecid
-
IC50: 17 mM
Rose bengal
-
IC50: 0.05 mM
sodium nitroprusside
-
in hepatic ischemia-reperfusion injured rats
Sulfobromophthalein
-
IC50: 0.06 mM
Triphenyltin chloride
-
poor inhibitor
Tumor necrosis factor alpha
-
zymosan
-
increase in LTC4S activity during differentiation of monocytic Mono Mac 6 cells by presence of leukotriene A4 is reduced by 80% in the presence of zymosan. Treatment with Zymosan for 48 h similarly attenuates LTC4S activity of primary human monocyte-derived macrophages and dendritic cells
-
additional information
-
cell treatment with ERK 1/2 specific inhibitor 1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene (U0126) blocks LTC4S expression, pyrrolidine dithiocarbamate inhibits reactive oxygen species generation and NF-?B activation, which in turn blocks LTC4S expression
-