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Literature summary for 2.4.1.17 extracted from

  • Nishimura, Y.; Maeda, S.; Ikushiro, S.; Mackenzie, P.I.; Ishii, Y.; Yamada, H.
    Inhibitory effects of adenine nucleotides and related substances on UDP-glucuronosyltransferase: Structure-effect relationships and evidence for an allosteric mechanism (2007), Biochim. Biophys. Acta, 1770, 1557-1566.
    View publication on PubMed

General Stability

General Stability Organism
phosphatidylcholine stabilizes the detergent treated enzyme Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
ADP markedly reduces 4-methylumbelliferone UGT activity only when detergent-treated rat liver microsomes are used as the enzyme source, inhibits UGT activity non-competitively without competing with either 4-methylumbelliferone or UDP-D-glucuronic acid Rattus norvegicus
AMP inhibits exclusively the estradiol 17-glucuronidation activity Rattus norvegicus
ATP markedly reduces 4-methylumbelliferone UGT activity only when detergent-treated rat liver microsomes are used as the enzyme source, inhibits UGT activity non-competitively without competing with either 4-methylumbelliferone or UDP-D-glucuronic acid Rattus norvegicus
CTP no inhibition of UGT by other cytosine-related nucleotides but CTP Rattus norvegicus
GTP weak inhibition, no inhibition of UGT by other guanosine-related nucleotides but GTP Rattus norvegicus
additional information AMP antagonizes the inhibitory effects of adenine, ATP, and NADP+ on 4-methylumbelliferone and estradiol 3-glucuronidation activities, no inhibition by glucose 1-phosphate, glucose 6-phosphate, fructose 1-phosphate, and fructose 6-phosphate, and by cytidine, dCTP, cytosine, CMP, dGTP, guanosine, GDP, GMP, NADH, NADPH, dATP, and adenosine Rattus norvegicus
NAD+ inhibits UGT activity non-competitively without competing with either 4-methylumbelliferone or UDP-D-glucuronic acid Rattus norvegicus
NADP+ markedly reduces 4-methylumbelliferone UGT activity only when detergent-treated rat liver microsomes are used as the enzyme source, inhibits UGT activity non-competitively without competing with either 4-methylumbelliferone or UDP-D-glucuronic acid Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
endoplasmic reticulum membrane
-
Rattus norvegicus 5789
-
microsome
-
Rattus norvegicus
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
UDP-D-glucuronate + acceptor Rattus norvegicus
-
UDP + acceptor beta-D-glucuronoside
-
?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
native enzyme partially by microsome preparation Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-D-glucuronate + 4-methylumbelliferone
-
Rattus norvegicus UDP + 4-methylumbelliferyl beta-D-glucuronoside
-
?
UDP-D-glucuronate + acceptor
-
Rattus norvegicus UDP + acceptor beta-D-glucuronoside
-
?
UDP-D-glucuronate + estradiol
-
Rattus norvegicus UDP + estradiol-3-beta-D-glucuronoside
-
?

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase
-
Rattus norvegicus
UGT
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.1
-
assay at Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics, overview Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0059
-
pH 7.1, 37°C, inhibition of 4-methylumbelliferone glucuronidation activity Rattus norvegicus CTP
0.008
-
pH 7.1, 37°C, inhibition of estradiol 17-glucuronidation activity Rattus norvegicus NADP+
0.009
-
pH 7.1, 37°C, inhibition of 4-methylumbelliferone glucuronidation activity Rattus norvegicus NAD+
0.01
-
pH 7.1, 37°C, inhibition of 4-methylumbelliferone glucuronidation activity Rattus norvegicus NADP+
0.0117
-
pH 7.1, 37°C, inhibition of estradiol 17-glucuronidation activity Rattus norvegicus ATP
0.0118
-
pH 7.1, 37°C, inhibition of estradiol 17-glucuronidation activity Rattus norvegicus NAD+
0.0154
-
pH 7.1, 37°C, inhibition of 4-methylumbelliferone glucuronidation activity Rattus norvegicus ATP
0.0252
-
pH 7.1, 37°C, inhibition of estradiol 3-glucuronidation activity Rattus norvegicus NADP+
0.0259
-
pH 7.1, 37°C, inhibition of 4-methylumbelliferone glucuronidation activity Rattus norvegicus ADP
0.0272
-
pH 7.1, 37°C, inhibition of estradiol 17-glucuronidation activity Rattus norvegicus ADP
0.031
-
pH 7.1, 37°C, inhibition of estradiol 17-glucuronidation activity Rattus norvegicus AMP
0.0321
-
pH 7.1, 37°C, inhibition of estradiol 3-glucuronidation activity Rattus norvegicus NAD+
0.0347
-
pH 7.1, 37°C, inhibition of estradiol 17-glucuronidation activity Rattus norvegicus CTP
0.0352
-
pH 7.1, 37°C, inhibition of estradiol 3-glucuronidation activity Rattus norvegicus ATP
0.0558
-
pH 7.1, 37°C, inhibition of estradiol 3-glucuronidation activity Rattus norvegicus CTP
0.0774
-
pH 7.1, 37°C, inhibition of estradiol 3-glucuronidation activity Rattus norvegicus ADP
0.108
-
pH 7.1, 37°C, inhibition of 4-methylumbelliferone glucuronidation activity Rattus norvegicus GTP
0.129
-
pH 7.1, 37°C, inhibition of estradiol 17-glucuronidation activity Rattus norvegicus GTP
0.227
-
pH 7.1, 37°C, inhibition of estradiol 3-glucuronidation activity Rattus norvegicus GTP