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Literature summary for 2.4.1.17 extracted from

  • Patana, A.S.; Kurkela, M.; Goldman, A.; Finel, M.
    The human UDP-glucuronosyltransferase: identification of key residues within the nucleotide-sugar binding site (2007), Mol. Pharmacol., 72, 604-611.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant isozymes as C-terminal Histagged fusion proteins in baculovirus-infected insect cells, expression levels, overview Homo sapiens

Protein Variants

Protein Variants Comment Organism
H369A site-directed mutagenesis of isozyme UGT1A9, the Km values for scopoletin and UDP-D-glucuronate are increased compared to the wild-type isozyme, the mutant shows impaired cosubstrate binding Homo sapiens
H371A site-directed mutagenesis of isozyme UGT1A6, the Km values for scopoletin and UDP-D-glucuronate are increased by 4 and 11fold, respectively, compared to the wild-type isozyme, the mutant shows severely impaired cosubstrate binding Homo sapiens
H377A site-directed mutagenesis of isozyme UGT1A9, inactive mutant Homo sapiens
H379A site-directed mutagenesis of isozyme UGT1A6, the Km values for scopoletin and UDP-D-glucuronate are increased compared to the wild-type isozyme, the mutant shows severely impaired cosubstrate binding Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information bisubstrate kinetics of wild-type and mutant isozyme UGT1A6 Homo sapiens
0.048
-
1-naphthol H379A mutant isozyme UGT1A6 Homo sapiens
0.08
-
scopoletin wild-type isozyme UGT1A9 Homo sapiens
0.083
-
1-naphthol H371A mutant isozyme UGT1A6 Homo sapiens
0.17
-
4-Methylumbelliferone wild-type isozyme UGT1A6 Homo sapiens
0.29
-
scopoletin wild-type isozyme UGT1A6 Homo sapiens
0.58
-
4-Methylumbelliferone H379A mutant isozyme UGT1A6 Homo sapiens
0.66
-
4-Methylumbelliferone H371A mutant isozyme UGT1A6 Homo sapiens
1.64
-
scopoletin H369A mutant isozyme UGT1A9 Homo sapiens
3.88
-
scopoletin H371A mutant isozyme UGT1A6 Homo sapiens
7.64
-
scopoletin H379A mutant isozyme UGT1A6 Homo sapiens
27
-
1-naphthol wild-type isozyme UGT1A6 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
endoplasmic reticulum membrane
-
Homo sapiens 5789
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
UDP-D-glucuronate + acceptor Homo sapiens UDP-glucuronosyltransferases play important roles in the metabolism, detoxification,and clearance of many different xenobiotics, including drugs and endogenous compounds UDP + acceptor beta-D-glucuronoside
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozyme UGT1A6
-

Reaction

Reaction Comment Organism Reaction ID
UDP-alpha-D-glucuronate + acceptor = UDP + acceptor beta-D-glucuronoside compulsory ordered bi bi mechanism Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-D-glucuronate + 1-naphthol
-
Homo sapiens UDP + 1-naphthyl beta-D-glucuronoside
-
?
UDP-D-glucuronate + 4-methylumbelliferone
-
Homo sapiens UDP + 4-methylumbelliferyl beta-D-glucuronoside
-
?
UDP-D-glucuronate + acceptor
-
Homo sapiens UDP + acceptor beta-D-glucuronoside
-
?
UDP-D-glucuronate + acceptor UDP-glucuronosyltransferases play important roles in the metabolism, detoxification,and clearance of many different xenobiotics, including drugs and endogenous compounds Homo sapiens UDP + acceptor beta-D-glucuronoside
-
?
UDP-D-glucuronate + scopoletin substrate binding structure, UGT1A6 residues His371 and Glu379 are directly involved in UDPGA binding but are not the general acid or general base, homology mocelling, overview Homo sapiens UDP + scopoletin beta-D-glucuronoside
-
?
UDP-D-glucuronate + umbelliferone
-
Homo sapiens UDP + umbelliferyl beta-D-glucuronoside
-
?

Subunits

Subunits Comment Organism
More substrate binding structure, homology mnodelling of wild-type and mutant isozymes UGT1A6 and UGT1A9, overview Homo sapiens

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase
-
Homo sapiens
UGT
-
Homo sapiens