Information on EC 2.4.1.95 - bilirubin-glucuronoside glucuronosyltransferase

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The expected taxonomic range for this enzyme is: Euarchontoglires

EC NUMBER
COMMENTARY hide
2.4.1.95
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RECOMMENDED NAME
GeneOntology No.
bilirubin-glucuronoside glucuronosyltransferase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
2 bilirubin-glucuronoside = bilirubin + bilirubin-bisglucuronoside
show the reaction diagram
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glucuronyl group transfer
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hexosyl group transfer
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SYSTEMATIC NAME
IUBMB Comments
bilirubin-glucuronoside:bilirubin-glucuronoside D-glucuronosyltransferase
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CAS REGISTRY NUMBER
COMMENTARY hide
71822-22-5
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
Wistar
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Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
metabolism
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
acetaminophen + UDP-glucuronate
?
show the reaction diagram
-
-
-
?
bilirubin monoglucuronide + bilirubin monoglucuronide
bilirubin diglucuronide + bilirubin
show the reaction diagram
serotonin + UDP-glucuronate
UDP + 3-(2-aminoethyl)-1H-indol-5-yl beta-D-glucuronide
show the reaction diagram
-
-
-
?
UDP-glucuronate + 1-naphthol
UDP + beta-D-glucuronosyl-(1-naphthol)
show the reaction diagram
-
-
-
?
UDP-glucuronate + 4-methylumbelliferone
UDP + beta-D-glucuronosyl-(4-methylumbelliferone)
show the reaction diagram
-
-
-
?
UDP-glucuronate + 4-nitrophenol
UDP + 4-nitrophenol beta-D-glucuronide
show the reaction diagram
-
-
-
?
UDP-glucuronate + buprenorphine
UDP + buprenorphine glucuronide
show the reaction diagram
-
-
-
?
UDP-glucuronic acid + bilirubin
bilirubin glucuronoside + UDP
show the reaction diagram
UDP-glucuronic acid + bilirubin
UDP + bilirubin O-glucuronide
show the reaction diagram
-
-
-
-
?
UDP-glucuronic acid + diclofenac
UDP + diclofenac O-glucuronide
show the reaction diagram
-
-
-
-
?
UDP-glucuronic acid + estradiol
UDP + estradiol 3-O-glucuronide
show the reaction diagram
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-
-
-
?
UDP-glucuronic acid + imipramine
UDP + imipramine N-glucuronide
show the reaction diagram
-
-
-
-
?
UDP-glucuronic acid + serotonin
UDP + serotonin O-glucuronide
show the reaction diagram
-
-
-
-
?
UDP-glucuronic acid + trifluoperazine
UDP + trifluoperazine N-glucuronide
show the reaction diagram
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-
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-
?
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mg2+
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INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-naphthol
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4-hydroxyphenytoin
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4-Methylumbelliferone
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7-ethyl-10-hydroxycamptothecin
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weak inhibitor of bilirubin glucuronidation
anthraflavic acid
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baicalein
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carvedilol
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daidzein
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ethinylestradiol
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Farnesol
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ketoconazole
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levothyroxine
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niflumic acid
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raltegravir
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riluzole
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ritonavir
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SN-38
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.02
bilirubin
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in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.033 - 0.035
bilirubin monoglucuronide
additional information
additional information
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coexpression of UGT1A4 and UGT1A6 decrease the S50 and Vmax values of UGT1A1-catalyzed estradiol 3-O-glucuronide formation and increase the Vmax value of UGT1A1-catalyzed bilirubin O-glucuronide formation; estradiol 3-O-formation: Vmax (pmol/min/unit): 975, 498.4 (1A1 co-expressed with isoform 1A4), 917 (1A1 co-expressed with isoform 1A6). Billirubin O-glucuronide formation: 223.5, 256.3 (1A1 co-expressed with isoform 1A4), 303.7 (1A1 co-expressed with isoform 1A6)
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.24
1-naphthol
Homo sapiens
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in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.12
4-hydroxyphenytoin
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.1
4-Methylumbelliferone
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.3564
7-ethyl-10-hydroxycamptothecin
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.0036
anthraflavic acid
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.007
baicalein
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.027
carvedilol
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.0073
daidzein
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.021
ethinylestradiol
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.047
Farnesol
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.027
ketoconazole
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.0049
levothyroxine
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.053
niflumic acid
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.17
raltegravir
Homo sapiens
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.18
riluzole
Homo sapiens
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in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.003
ritonavir
Homo sapiens
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in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.36
SN-38
Homo sapiens
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in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
50000
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SDS-PAGE, each UGT1A isoform shows a single band at 50 to 55 kDa, owing to the differences in the levels of glycosylation
160000
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gel filtration
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
following incubation of solubilized plasma membrane with pronase at 37C for 180 min, 80% of enzyme activity is lost
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Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expressed in HEK293 cells
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expressed in HEK293 cells; expressed in HEK293 cells; expressed in HEK293 cells; expressed in HEK293 cells; expressed in HEK293 cells; expressed in HEK293 cells; expressed in HEK293 cells; expressed in HEK293 cells; expressed in HEK293 cells; expressed in HEK293 cells; expressed in HEK293 cells
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
F83L
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the mutant exhibits less than 5% of wild type conjugation capacity
G211A
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subtype *6, subtype *6/*6 is related to hyperbilirubinemia, diplotypes of compound haplotypes (*60/*6 and wild-type/*60 + wild-type/*28 + wild-type/*6) are significantly related to hyperbilirubinemia development
G71R
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the mutant exhibits about 30% of wild type conjugation capacity
I294T
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the mutant exhibits about 40% of wild type conjugation capacity
N400D
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the mutant exhibits about 60% of wild type conjugation capacity
R336L
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the mutant exhibits about 80% of wild type conjugation capacity
T3279G
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subtype *60, diplotypes of this subtype plus subtype *28 (*60/*60 + *28/*28) are only found in hyperbilirubinemic patients, they show highest bilirubin concentrations, this variant is not found in controls, diplotypes of compound haplotypes (*60/*28, *60/6, wild-type/*60 + wild-type/*28 + wild-type/*6) are significantly related to hyperbilirubinemia development, also *60/*60 and *60/*60 + wild-type/*28 are related to hyperbilirubinemia
W461R
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the mutant exhibits less than 5% of wild type conjugation capacity
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine