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Literature summary for 2.4.1.17 extracted from

  • Mano, Y.; Usui, T.; Kamimura, H.
    Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes (2007), Basic Clin. Pharmacol. Toxicol., 101, 211-214.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
17alpha-ethynylestradiol slightly activates the 3-beta-glucuronidation of estradiol to 116% at 0.005 mM, but inhibits it at 0.1 mM by 23% Homo sapiens
propofol activates the glucuronidation of 4-methylumbelliferone at 0.2 mM leading to 1.5fold increased Vmax and 0.53fold reduced Km, overview Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
17alpha-ethynylestradiol slightly activates the 3-beta-glucuronidation of estradiol to 116% at 0.005 mM, but inhibits it at 0.1 mM by 23%, inhibits glucuronidation of 4-methylumbelliferone at all concentration of 0.1 mM Homo sapiens
propofol inhibits 3-beta-glucuronidation of estradiol by recombinant isozyme UGT1A1 and by liver microsomes Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.054
-
4-Methylumbelliferone pH 7.5, 37°C, 0.2 mM propofol, isozyme UGT1A1 Homo sapiens
0.101
-
4-Methylumbelliferone pH 7.5, 37°C, isozyme UGT1A1 Homo sapiens

Localization

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
UDP-D-glucuronate + acceptor Homo sapiens
-
UDP + acceptor beta-D-glucuronoside
-
?
UDP-D-glucuronate + estradiol Homo sapiens liver microsomes UDP + estradiol-3-beta-D-glucuronoside
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P22309 isozyme UGT1A1; isozyme UGT1A1
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-D-glucuronate + 4-methylumbelliferone recombinant isozyme UGT1A1 Homo sapiens UDP + 4-methylumbelliferyl beta-D-glucuronoside
-
?
UDP-D-glucuronate + acceptor
-
Homo sapiens UDP + acceptor beta-D-glucuronoside
-
?
UDP-D-glucuronate + estradiol liver microsomes Homo sapiens UDP + estradiol-3-beta-D-glucuronoside
-
?
UDP-D-glucuronate + estradiol recombinant isozyme UGT1A1 Homo sapiens UDP + estradiol-3-beta-D-glucuronoside
-
?

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase
-
Homo sapiens
UGT1A1
-
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
7.5
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0086
-
pH 7.5, 37°C, inhibition of glucuronidation of 4-methylumbelliferone by isozyme UGT1A1 Homo sapiens 17alpha-ethynylestradiol
0.059
-
pH 7.5, 37°C, inhibition of 3-beta-glucuronidation of estradiol by recombinant isozyme UGT1A1 Homo sapiens propofol
0.228
-
pH 7.5, 37°C, inhibition of 3-beta-glucuronidation of estradiol by liver microsomes Homo sapiens propofol