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Literature summary for 2.4.1.17 extracted from

  • Yuan, L.; Qian, S.; Xiao, Y.; Sun, H.; Zeng, S.
    Homo- and hetero-dimerization of human UDP-glucuronosyltransferase 2B7 (UGT2B7) wild type and its allelic variants affect zidovudine glucuronidation activity (2015), Biochem. Pharmacol., 95, 58-70.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
gene UGT2B7, DNA and amino acid sequence determination and analysis, genotyping, three non-synonymous single nucleotide polymorphisms are identified, expression of CFP-tagged, YFP-tagged and HA-tagged UGT2B7 wild-type and mutant allozymes in Spodoptera frugiperda Sf9 cells via baculovirus transfection Homo sapiens

Protein Variants

Protein Variants Comment Organism
A71S naturally occuring mutation, non-synonymous single nucleotide polymorphism Homo sapiens
D398N naturally occuring mutation, non-synonymous single nucleotide polymorphism Homo sapiens
H268Y naturally occuring mutation, non-synonymous single nucleotide polymorphism Homo sapiens
additional information protein-protein interactions among UGT2B7 allozymes wild-type, A71S, H268Y and D398N, by performing a systematic quantitative fluorescence resonance energy transfer (FRET) analysis in combination with co-immunoprecipitation assay, UGT2B7 allozymes form homo- and hetero-dimers and show distinct features in donor-acceptor distances. Both codon 71 and codon 268 in the N-terminal domain are involved in the dimeric interaction. Coimmunoprecipitation experiments also prove that UGT2B7 allozymes form stable dimers. An increase in activity is observed when wild-type hetero-dimerized with A71S compared with homo-dimers, while both H268Y and D398N impair the activity of WT and A71S by forming hetero-dimers. In addition, zidovudine glucuronidation activity is associated with FRET distance Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.508
-
zidovudine pH 7.4, 37°C, recombinant HA-tagged wild-type dimer Homo sapiens
0.519
-
zidovudine pH 7.4, 37°C, recombinant CFP-tagged mutant H268Y dimer Homo sapiens
0.534
-
zidovudine pH 7.4, 37°C, recombinant HA-tagged mutant A71S dimer Homo sapiens
0.54
-
zidovudine pH 7.4, 37°C, recombinant dimer of CFP-tagged H268Y and HA-tagged D398N mutant monomers Homo sapiens
0.57
-
zidovudine pH 7.4, 37°C, recombinant HA-tagged mutant H268Y dimer Homo sapiens
0.589
-
zidovudine pH 7.4, 37°C, recombinant dimer of CFP-tagged A71S and HA-tagged D398N mutant monomers Homo sapiens
0.605
-
zidovudine pH 7.4, 37°C, recombinant CFP-tagged wild-type dimer Homo sapiens
0.605
-
zidovudine pH 7.4, 37°C, recombinant dimer of CFP-tagged wild-type and HA-tagged D398N mutant monomers Homo sapiens
0.609
-
zidovudine pH 7.4, 37°C, recombinant dimer of CFP-tagged A71S and HA-tagged H268Y mutant monomers Homo sapiens
0.634
-
zidovudine pH 7.4, 37°C, recombinant CFP-tagged mutant A71S dimer Homo sapiens
0.706
-
zidovudine pH 7.4, 37°C, recombinant dimer of CFP-tagged wild-type and HA-tagged A71S mutant monomers Homo sapiens
0.841
-
zidovudine pH 7.4, 37°C, recombinant dimer of CFP-tagged wild-type and HA-tagged H268Y mutant monomers Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Homo sapiens 16020
-
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.
UDP-glucuronate + estriol Homo sapiens
-
UDP + estriol beta-D-glucuronoside
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P16662 gene UGT2B7
-

Purification (Commentary)

Purification (Comment) Organism
HA-tagged UGT2B7 wild-type and mutant allozymes in Spodoptera frugiperda Sf9 cells by hemagglutinin immunoaffinity chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-glucuronate + estriol
-
Homo sapiens UDP + estriol beta-D-glucuronoside
-
?
UDP-glucuronate + zidovudine
-
Homo sapiens UDP + zidovudine O-beta-D-glucuronoside
-
?

Subunits

Subunits Comment Organism
More UGT2B7 forms oligomers that affect its enzymatic activity. Protein–protein interactions among UGT2B7 allozymes wild-type, A71S, H268Y and D398N, by performing a systematic quantitative fluorescence resonance energy transfer (FRET) analysis in combination with co-immunoprecipitation assay, UGT2B7 allozymes form homo- and hetero-dimers and show distinct features in donor–acceptor distances. Both codon 71 and codon 268 in the N-terminal domain are involved in the dimeric interaction. Coimmunoprecipitation experiments also prove that UGT2B7 allozymes form stable dimers Homo sapiens

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase 2B7
-
Homo sapiens
UGT2B7
-
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

General Information

General Information Comment Organism
physiological function UGT2B7 is one of the most important UGTs that glucuronidates abundant endobiotics and xenobiotics, such as estriol, morphine, and anticancer drugs Homo sapiens