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Literature summary for 1.13.11.11 extracted from

  • Sari, S.; Tomek, P.; Leung, E.; Reynisson, J.
    Discovery and characterisation of dual inhibitors of tryptophan 2,3-dioxygenase (TDO2) and indoleamine 2,3-dioxygenase 1 (IDO1) using virtual screening (2019), Molecules, 24, 4346 .
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
1-(2-hydroxy-4-methylphenyl)-3-(2-methoxyphenyl)propane-1,3-dione
-
 Homo sapiens
1-(2-hydroxy-4-methylphenyl)-3-{2-[(propan-2-yl)oxy]phenyl}propane-1,3-dione
-
 Homo sapiens
1-(3-bromothiophen-2-yl)-2-(3-methyl-1,4-dihydronaphthalen-2-yl)ethan-1-one most potent inhibitor capable of blocking both indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO2) activity, with the IC50 value for BT-549 cells at 0.00342 mM Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-tryptophan + O2 Homo sapiens
-
 N-formyl-L-kynurenine
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P48775
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-172 cell
-
 Homo sapiens
-
BT-549 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-tryptophan + O2
-
 Homo sapiens N-formyl-L-kynurenine
-
 ?

Synonyms

Synonyms Comment Organism
TDO2
-
 Homo sapiens
tryptophan 2,3-dioxygenase
-
 Homo sapiens

General Information

General Information Comment Organism
physiological function the enzyme catalyses the rate-limiting step in the kynurenine pathway, an important biochemical mechanism for immunological responsecancers express tryptophan catabolising enzymes indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO2) to produce immunosuppressive tryptophan metabolites that undermine thr immune systems of patients, leading to poor disease outcomes Homo sapiens