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Literature summary for 2.6.1.7 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
Search for more literature for 2.6.1.7

Application

Application Comment Organism
analysis development of a coupled fluorescence assay for human KATII with short assay time Homo sapiens
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)

Cloned (Comment) Organism
expression in Sf9 cell Homo sapiens

Inhibitors

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

KM Value [mM]

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

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
-
 ?

Synonyms

Synonyms Comment Organism
KAT2
-
 Homo sapiens

Turnover Number [1/s]

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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
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]

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