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Literature summary extracted from

  • Lu, H.; Kopcho, L.; Ghosh, K.; Witmer, M.; Parker, M.; Gupta, S.; Paul, M.; Krishnamurthy, P.; Laksmaiah, B.; Xie, D.; Tredup, J.; Zhang, L.; Abell, L.M.
    Development of a RapidFire mass spectrometry assay and a fluorescence assay for the discovery of kynurenine aminotransferase II inhibitors to treat central nervous system disorders (2016), Anal. Biochem., 501, 56-65.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.6.1.7 analysis development of a coupled fluorescence assay for human KATII with short assay time Homo sapiens
2.6.1.7 analysis development of a sensitive, high-throughput, label-free RapidFire mass spectrometry assay for kynurenine aminotransferase. The method is directly applicable to KATII enzymes from different animal species, allowing to select proper animal model(s) to evaluate human KATII inhibitors Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.6.1.7 expression in Sf9 cell Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.6.1.7 (3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one
-
 Homo sapiens
2.6.1.7 (3S)-3-amino-6-benzyl-1-hydroxy-7-methoxy-3,4-dihydroquinolin-2(1H)-one
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.6.1.7 0.68
-
 L-kynurenine mass spectrometry assay, pH 7.5, temperature not specified in the publication Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.6.1.7 Homo sapiens Q8N5Z0
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.6.1.7 L-kynurenine + 2-oxoglutarate
-
 Homo sapiens 4-(2-aminophenyl)2,4-dioxobutanoate + L-glutamate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.6.1.7 KAT2
-
 Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.6.1.7 4.6
-
 L-kynurenine mass spectrometry assay, pH 7.5, temperature not specified in the publication Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.6.1.7 0.000004
-
 mass spectrometry assay, pH 7.5, temperature not specified in the publication Homo sapiens (3S)-3-amino-6-benzyl-1-hydroxy-7-methoxy-3,4-dihydroquinolin-2(1H)-one
2.6.1.7 0.000005
-
 fluorescence assay, pH 7.5, temperature not specified in the publication Homo sapiens (3S)-3-amino-6-benzyl-1-hydroxy-7-methoxy-3,4-dihydroquinolin-2(1H)-one
2.6.1.7 0.000015
-
 flourescence assay, pH 7.5, temperature not specified in the publication Homo sapiens (3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one
2.6.1.7 0.00003
-
 mass spectrometry assay, pH 7.5, temperature not specified in the publication Homo sapiens (3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
2.6.1.7 6.8
-
 L-kynurenine mass spectrometry assay, pH 7.5, temperature not specified in the publication Homo sapiens