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Literature summary for 2.4.1.17 extracted from

  • Starlard-Davenport, A.; Xiong, Y.; Bratton, S.; Gallus-Zawada, A.; Finel, M.; Radominska-Pandya, A.
    Phenylalanine(90) and phenylalanine(93) are crucial amino acids within the estrogen binding site of the human UDP-glucuronosyltransferase 1A10 (2007), Steroids, 72, 85-94.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.4.1.17

Cloned(Commentary)

Cloned (Comment) Organism
expression of UGT1A10 in baculovirus-infected Sf9 insect cells as His-tagged protein Homo sapiens

Protein Variants

Protein Variants Comment Organism
F90A exhibits little or no activity towards estrone, estradiol and estriol. Complete loss of activity with 2-hydroxyestrone, 2-hydroxyestradiol, 4-hydroxyestradiol and 4-hydroxyestrone Homo sapiens
F90L 86% decrease in activity towards estrone, increase in affinity. Decrease in catalytic activity toward estradiol of 64%, and an almost 3fold increase in affinity. Estriol is not glucuronated by the mutant enzyme. 72% increase in activity towards 2-hydroxyestrone. 78% decrease in activity towards 4-hydroxyestrone. Increase in activity towards 4-hydroxyestradiol Homo sapiens
F93A 75% decrease in activity towards estrone. For estradiol, the F93A mutant showes a slight impairment of activity with 30% decrease in Vmax. The Km for estradiol decreases approximately 2fold. 59% decrease in activity towards estriol, similar KM-value. 99% decrease in activity towards 2-hydroxyestrone. 69% decrease in activity towards 4-hydroxyestrone, increase in affinity. 93% decrease in activity topwards 4-hydroxyestradiol, increase in affinity Homo sapiens
F93L exhibits little or no activity towards estrone, estradiol and estriol. 88% decrease in activity towards 2-hydroxyestrone, increase in affinity. Complete loss in activity towards 4-hydroxyestrone and 4-hydroxyestradiol Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0049
-
 estradiol 37°C, pH 8.0, mutant enzyme F90L Homo sapiens
0.0063
-
 estrone 37°C, pH 8.0, mutant enzyme F93A Homo sapiens
0.0078
-
 estradiol 37°C, pH 8.0, mutant enzyme F93A Homo sapiens
0.0102
-
 2-hydroxyestrone 37°C, pH 8.0, mutant enzyme F93A Homo sapiens
0.0138
-
 estradiol 37°C, pH 8.0, wild-type enzyme Homo sapiens
0.0388
-
 estriol 37°C, pH 8.0, wild-type enzyme Homo sapiens
0.0401
-
 4-hydroxyestradiol 37°C, pH 8.0, mutant enzyme F93A Homo sapiens
0.0401
-
 4-hydroxyestrone 37°C, pH 8.0, mutant enzyme F93A Homo sapiens
0.0421
-
 estrone 37°C, pH 8.0, wild-type enzyme Homo sapiens
0.0467
-
 estriol 37°C, pH 8.0, mutant enzyme F93A Homo sapiens
0.0823
-
 2-hydroxyestrone 37°C, pH 8.0, mutant enzyme F93L Homo sapiens
0.1182
-
 4-hydroxyestrone 37°C, pH 8.0, wild-type enzyme Homo sapiens
0.1305
-
 2-hydroxyestrone 37°C, pH 8.0, wild-type enzyme Homo sapiens
0.2338
-
 4-hydroxyestradiol 37°C, pH 8.0, wild-type enzyme Homo sapiens
0.291
-
 2-hydroxyestrone 37°C, pH 8.0, mutant enzyme F90L Homo sapiens
0.292
-
 4-hydroxyestradiol 37°C, pH 8.0, mutant enzyme F90L 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.
estrogen + UDP-glucuronate Homo sapiens UDP-glucuronosyltransferase 1A10 has been identified as the major isoform involved in the biotransformation of a wide range of phenolic substrates, including native estrogens and their oxidized metabolites ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9HAW8
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-hydroxyestradiol + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
2-hydroxyestrone + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
4-hydroxyestradiol + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
4-hydroxyestrone + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
estradiol + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
estriol + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
estrogen + UDP-glucuronate UDP-glucuronosyltransferase 1A10 has been identified as the major isoform involved in the biotransformation of a wide range of phenolic substrates, including native estrogens and their oxidized metabolites Homo sapiens ?
-
 ?
estrogen + UDP-glucuronate phenylalanine(90) and phenylalanine(93) are crucial amino acids within the estrogen binding site of the human UDP-glucuronosyltransferase 1A10 Homo sapiens ?
-
 ?
estrone + UDP-glucuronate
-
 Homo sapiens UDP + estrone 3-O-glucuronide
-
 ?

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase 1A10
-
 Homo sapiens