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Literature summary for 1.8.1.9 extracted from

  • Ren, X.; Zou, L.; Lu, J.; Holmgren, A.
    Selenocysteine in mammalian thioredoxin reductase and application of ebselen as a therapeutic (2018), Free Radic. Biol. Med., 127, 238-247 .
    View publication on PubMed
Search for more literature for 1.8.1.9

Inhibitors

Inhibitors Comment Organism Structure
ebselen reversible competitive inhibitor of the enzyme from Escherichia coli. Ebselen can form a stable selenosulfide bond with the attacking cysteine in Escherichia coli thioredoxin reductase which cannot easily be resolved by the other cysteine in the active site. The binding blocks the electron transfer from Escherichia coli TrxR to Trx, and ultimately to the downstream substrates of thioredoxin. Ebselen is an excellent substrate for mammalian thioredoxin system Escherichia coli

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
 Homo sapiens 5739
-

Metals/Ions

Metals/Ions Comment Organism Structure
selenium contains a selenocysteine in its active site Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
thioredoxin disulfide + NADPH + H+ Escherichia coli
-
 thioredoxin + NADP+
-
 ?
thioredoxin disulfide + NADPH + H+ Homo sapiens the enzyme (TrxR) can use NADPH to reduce thioredoxin disulfide which passes the reducing equivalent to its downstream substrates involved in various biomedical events, such as ribonucleotide reductase for deoxyribonucleotide and DNA synthesis, or peroxiredoxins for counteracting oxidative stress thioredoxin + NADP+
-
 ?

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Homo sapiens Q86VQ6
-
-
Homo sapiens Q9NNW7
-
-

Source Tissue

Source Tissue Comment Organism Textmining
testis
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
thioredoxin disulfide + NADPH + H+
-
 Escherichia coli thioredoxin + NADP+
-
 ?
thioredoxin disulfide + NADPH + H+ the enzyme (TrxR) can use NADPH to reduce thioredoxin disulfide which passes the reducing equivalent to its downstream substrates involved in various biomedical events, such as ribonucleotide reductase for deoxyribonucleotide and DNA synthesis, or peroxiredoxins for counteracting oxidative stress Homo sapiens thioredoxin + NADP+
-
 ?
thioredoxin disulfide + NADPH + H+ ebselen is an excellent substrate for mammalian Trx system Homo sapiens thioredoxin + NADP+
-
 ?
thioredoxin disulfide + NADPH + H+ the active site of Escherichia coli thioredoxin reductase contains a CATC motif without any selenocysteine and it specifically reduces oxidized Escherichia coli thioredoxin Escherichia coli thioredoxin + NADP+
-
 ?

Subunits

Subunits Comment Organism
homodimer
-
 Escherichia coli
homodimer
-
 Homo sapiens

Synonyms

Synonyms Comment Organism
TrxR
-
 Escherichia coli
TrxR
-
 Homo sapiens
Txnrd2
-
 Homo sapiens
TXNRD3
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00052
-
 ebselen pH and temperature not specified in the publication Escherichia coli

General Information

General Information Comment Organism
drug target anti-cancer target. Selenocysteine is important for the biological functions of mammalian TrxR and distinguishes it from prokaryotic thioredoxin reductases. Therefore it is a promising drug target Homo sapiens
drug target ebselen as an inhibitor of thiol-dependent enzymes in pathogens Escherichia coli
physiological function the enzyme (TrxR) can use NADPH to reduce thioredoxin disulfide which passes the reducing equivalent to its downstream substrates involved in various biomedical events, such as ribonucleotide reductase for deoxyribonucleotide and DNA synthesis, or peroxiredoxins for counteracting oxidative stress Homo sapiens