1.8.1.B1: thioredoxin glutathione reductase
This is an abbreviated version!
For detailed information about thioredoxin glutathione reductase, go to the full flat file.
Word Map on EC 1.8.1.B1
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1.8.1.B1
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schistosoma
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schistosomiasis
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worm
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mansoni
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praziquantel
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glutaredoxin
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selenocysteine
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antischistosomal
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gssg
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auranofin
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platyhelminth
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flatworm
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dtnb
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fluke
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sjtgr
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fasciola
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oxadiazole
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cysticerci
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hysteretic
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medicine
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taenia
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trematode
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echinococcus
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granulosus
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schistosomicidal
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crassiceps
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gigantica
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selenocysteine-containing
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furoxans
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analysis
- 1.8.1.B1
- schistosoma
- schistosomiasis
- worm
- mansoni
- praziquantel
- glutaredoxin
- selenocysteine
-
antischistosomal
- gssg
- auranofin
-
platyhelminth
- flatworm
- dtnb
- fluke
-
sjtgr
- fasciola
-
oxadiazole
- cysticerci
-
hysteretic
- medicine
-
taenia
-
trematode
-
echinococcus
- granulosus
-
schistosomicidal
- crassiceps
- gigantica
-
selenocysteine-containing
- furoxans
- analysis
Reaction
Synonyms
cTGR, DmTrxR, EgTGR, mTGR, SmTGR, TGR, TGRsec, thioredoxin glutathione reductase, thioredoxin-glutathione reductase, thioredoxin/glutathione reductase
ECTree
1.8.1.B1 thioredoxin glutathione reductaseAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 1.8.1.B1 - thioredoxin glutathione reductase
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(2-oxido-1,2,5-oxadiazole-3,4-diyl)bis[(1,3-dimethyl-1H-pyrazol-4-yl)methanone]
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(2-oxido-1,2,5-oxadiazole-3,4-diyl)bis[(4-methoxyphenyl)methanone]
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(3R,5R,8R) 5-(((3-carboxy-4-nitrophenyl)disulfanyl)methyl)tetrahydro-2H-thiazolo[4,3-b]thiazole-3-carboxylic acid
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1,8-naphthyridine-2 carboxylate
mixed inhibition. 1,8-Naphthyridine-2 carboxylate prevents Tyr296 from rotating, a process necessary for NADPH binding and enzyme reduction. It inhibits by stabilizing a protein conformation whose affinity for NADPH is greatly reduced
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2-(4-chlorophenoxy)-6-methyl-2,3-dihydro-1,3,2-diazaphosphinin-4(1H)-one 2-oxide
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2-(4-ethoxyphenoxy)-6-methyl-2,3-dihydro-1,3,2-diazaphosphinin-4(1H)-one 2-oxide
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4-aminopiazthiole
inhibit the enzyme in a NADPH-dependent manner, and the inhibition appears to be irreversible even upon extensive dilution of the inhibited protein
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5-(((3-carboxy-4-nitrophenyl)disulfanyl)methyl) (2RS,5RS)-3,3a-dihydro-benzo[d]thiazolo[4,3-b]thiazole
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5-bromo-N-ethyl-3,4-dinitrothiophen-2-amine
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at 0.005 microM, 100 % larval death at 48 hours
5-chloro-N-[4-[ethyl(phenyl)sulfamoyl]phenyl]-2-(methanesulfonyl)pyrimidine-4-carboxamide
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6-methyl-2-phenoxy-2,3-dihydro-1,3,2-diazaphosphinin-4(1H)-one 2-oxide
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7-[(4-methoxyphenyl)[(4-methylpyridin-2-yl)amino]methyl]-2-methylquinolin-8-ol
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AuI-pyridine-2-thiol N-oxide
a potent inhibitor that achieves 75% inhibition at a 1:1 thioredoxin glutathione reductase:Au ratio and efficiently kills Echinococcus granulosus in vitro
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curcumin
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time-dependent process. An intermediary compound of curcumin oxidation, probably spiroepoxide, is responsible. Preincubation of curcumin in the presence of NADPH results in the loss of its inhibitory ability. Preincubation of curcumin with sulfhydryl compounds fully protected the enzyme from inhibition
diethyl 2-(3-bromo-6-oxo-6H-anthra[1,9-cd][1,2]oxazol-4-yl)-3-oxobutanedioate
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glutathione disulfide
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substrate inhibition at moderate or high concentrations. Noncompetitive mode of inhibition in which the disulfide behaves as an affinity label-like reagent through its binding and reduction at an alternative site, leading the enzyme into an inactive state
indole-3-carbinol
inhibit the enzyme in a NADPH-dependent manner, and the inhibition appears to be irreversible even upon extensive dilution of the inhibited protein
methyl (5-[1-[(tert-butoxycarbonyl)amino]-2-phenylethyl]-1,3,4-oxadiazole-2-sulfonyl)acetate
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NOC-7
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i.e. 1-hydroxy-2-oxo-3-(N-3-methyl-aminopropyl)-3-methyl-1-triazene, complete inhibition at 0.1 mM
P-1,3-benzothiazol-2-yl-N-(2-fluorophenyl)-P-phenylphosphinic amide
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P-1,3-benzothiazol-2-yl-N-(5-chloropyridin-2-yl)-P-phenylphosphinic amide
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P-1,3-benzothiazol-2-yl-P-phenyl-N-1,3-thiazol-2-ylphosphinic amide
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[mu-[1-(hydroxy-1kappaO)-2-(sulfanyl-1kappaS)pyridin-1-iumato(2-)]]-[mu-[1-(hydroxy-2kappaO)-2-(sulfanyl-1kappaS)pyridin-1-iumato(2-)]]bis(triphenylphosphane)digold
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a single gold atom binds to Cys519 and Cys573 in the AuI-enzyme complex. 7580% inhibition of thioredoxin and glutathione reductase activities is achieved at a 1:1 concentration ratio of inhibitor:enzyme
additional information
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the recombinant plasmid DNA vaccine pVAX1/SjTGR lowers enzymatic activity in vivo and in vitro
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1,3,4-oxadiazole-2-sulfone
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration
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1,3,4-oxadiazole-2-sulfone
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration
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1,3,4-oxadiazole-2-sulfone
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration
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2-((4-chlorophenyl)sulfonal)-6-methoxy-3-nitropyridine
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. Kills schistosomes within 1 h of administration
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2-((4-chlorophenyl)sulfonal)-6-methoxy-3-nitropyridine
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. Kills schistosomes within 1 h of administration
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2-((4-chlorophenyl)sulfonal)-6-methoxy-3-nitropyridine
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. Kills schistosomes within 1 h of administration
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4-chloro-5-[4-(hydroxymethyl)-1H-1,2,3-triazol-1-yl]-2-phenylpyridazin-3(2H)-one
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at 0.010 microM, 100 % larval death at 48 hours
4-chloro-5-[4-(hydroxymethyl)-1H-1,2,3-triazol-1-yl]-2-phenylpyridazin-3(2H)-one
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6-nitro-1H-1-benzothiophene-1,1-dione
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at 0.010 microM, 100 % larval death at 48 hours
6-nitrobenzo[b]thiophene-1,1-dioxide
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration
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6-nitrobenzo[b]thiophene-1,1-dioxide
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration
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6-nitrobenzo[b]thiophene-1,1-dioxide
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration
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auranofin
inhibition in a dose-dependent manner. The inhibitor expresses a lethal toxic effect on both newly excysted juveniles and adult worms of Opisthorchis viverrini in vitro
auranofin
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auranofin at 0.005 mg/ml (0.0074 mM) reduces 57.1% of the thioredoxin reductase activity and 71% of the glutathione reductase activity in the Schistosoma japonicum adult worms
auranofin
very potent inhibitor, nearly compete inhibition at 0.01 mM
pyrazine-3-one
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration
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pyrazine-3-one
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration
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pyrazine-3-one
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shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration
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