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Literature summary for 2.6.1.7 extracted from

  • Jayawickrama, G.; Nematollahi, A.; Sun, G.; Church, W.
    Improvement of kynurenine aminotransferase-II inhibitors guided by mimicking sulfate esters (2018), PLoS ONE, 13, e0196404 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.6.1.7

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Rosetta 2 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-(5,6-dichloro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanoic acid
-
 Homo sapiens
4-(5,6-dichloro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)benzenesulfonamide reversible inhibitor Homo sapiens
4-(5,6-dichloro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethylbenzenesulfonamide reversible inhibitor Homo sapiens
estradiol disulfate very strong inhibitor Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-kynurenine + 2-oxoglutarate Homo sapiens
-
 4-(2-aminophenyl)-2,4-dioxobutanoate + L-glutamate + H2O
-
 ir

Organism

Organism UniProt Comment Textmining
Homo sapiens Q8N5Z0
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-kynurenine + 2-oxoglutarate
-
 Homo sapiens 4-(2-aminophenyl)-2,4-dioxobutanoate + L-glutamate + H2O
-
 ir

Synonyms

Synonyms Comment Organism
KAT-II isoform Homo sapiens
kynurenine aminotransferase
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
pyridoxal 5'-phosphate
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0263
-
 at pH 7.4 and 37°C Homo sapiens estradiol disulfate
0.0738
-
 at pH 7.4 and 37°C Homo sapiens 4-(5,6-dichloro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)benzenesulfonamide
0.1128
-
 at pH 7.4 and 37°C Homo sapiens 4-(5,6-dichloro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethylbenzenesulfonamide
0.315
-
 at pH 7.4 and 37°C Homo sapiens (2R)-2-(5,6-dichloro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanoic acid