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Literature summary for 2.7.1.171 extracted from

  • Inaba, S.I.; Yamaguchi-Goto, M.; Tanaka-Takanaka, K.; Yonesu, K.; Sakurai, H.; Kubota, K.; Izumi, T.
    Enzymatic kinetics regarding reversible metabolism of CS-0777, a sphingosine 1-phosphate receptor modulator, via phosphorylation and dephosphorylation in humans (2018), Xenobiotica, 48, 258-268 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-deoxy-1-morpholinofructose DMF, a selective FN3K inhibitor, inhibits CS-0777 phosphorylation in erythrocytes by about 20% Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information Michaelis-Menten kinetics Homo sapiens
0.922
-
(R)-1-(5-(3-amino-4-hydroxy-3-methylbutyl)-1-methyl-1H-pyrrol-2-yl)-4-(p-tolyl)butan-1-one pH 7.4, 37°C, recombinant enzyme FN3K Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + (R)-1-(5-(3-amino-4-hydroxy-3-methylbutyl)-1-methyl-1H-pyrrol-2-yl)-4-(p-tolyl)butan-1-one Homo sapiens CS-0777 ADP + (2R)-2-amino-2-methyl-4-(1-methyl)-5-[4-(4-methylphenyl)butanoyl]-1H-pyrrol-2-yl)butyl dihydrogen phosphate
-
ir
ATP + [protein]-N6-D-fructosyl-L-lysine Homo sapiens
-
ADP + [protein]-N6-(3-O-phospho-D-fructosyl)-L-lysine
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9H479
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood platelet
-
Homo sapiens
-
erythrocyte
-
Homo sapiens
-
kidney
-
Homo sapiens
-
liver
-
Homo sapiens
-
lung
-
Homo sapiens
-
small intestine
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + (R)-1-(5-(3-amino-4-hydroxy-3-methylbutyl)-1-methyl-1H-pyrrol-2-yl)-4-(p-tolyl)butan-1-one CS-0777 Homo sapiens ADP + (2R)-2-amino-2-methyl-4-(1-methyl)-5-[4-(4-methylphenyl)butanoyl]-1H-pyrrol-2-yl)butyl dihydrogen phosphate
-
ir
ATP + [protein]-N6-D-fructosyl-L-lysine
-
Homo sapiens ADP + [protein]-N6-(3-O-phospho-D-fructosyl)-L-lysine
-
?

Synonyms

Synonyms Comment Organism
FN3K
-
Homo sapiens
fructosamine 3-kinase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

General Information

General Information Comment Organism
physiological function CS-0777, a candidate compound for autoimmune diseases, becomes phosphorylated to an active metabolite, M1, by fructosamine 3-kinase (FN3K) and FN3K-related protein (FN3K-RP, EC 2.7.1.172), and (2R)-2-amino-2-methyl-4-(1-methyl)-5-[4-(4-methylphenyl)butanoyl]-1H-pyrrol-2-yl)butyl dihydrogen phosphate is reverted back to CS-0777 by alkaline phosphatase (ALP) in the body Homo sapiens