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
2.4.1.95
-
RECOMMENDED NAME
GeneOntology No.
bilirubin-glucuronoside glucuronosyltransferase
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
2 bilirubin-glucuronoside = bilirubin + bilirubin-bisglucuronoside
show the reaction diagram
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glucuronyl group transfer
-
-
-
-
hexosyl group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
bilirubin-glucuronoside:bilirubin-glucuronoside D-glucuronosyltransferase
-
SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
bilirubin glucuronoside glucuronosyltransferase
-
-
-
-
bilirubin monoglucuronide transglucuronidase
-
-
-
-
glucuronosyltransferase, bilirubin glucuronoside
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
71822-22-5
-
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
sickle cell disease patients of the Bantu beta S haplotype, mean age 12.0
-
-
Manually annotated by BRENDA team
Taiwanese hyperbilirubinemia patients
-
-
Manually annotated by BRENDA team
Rattus norvegicus Wistar
Wistar
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
metabolism
-
bilirubin
metabolism
-
bilirubin metabolism
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
acetaminophen + UDP-glucuronate
?
show the reaction diagram
Q20CK6, Q20CK7, Q20CK8, Q20CK9, Q20CL0, Q20CL1, Q20CL2, Q20CL3, Q20CL4, Q20CL5, Q20CL6
-
-
-
?
bilirubin monoglucuronide + bilirubin monoglucuronide
bilirubin diglucuronide + bilirubin
show the reaction diagram
-
-
-
?
bilirubin monoglucuronide + bilirubin monoglucuronide
bilirubin diglucuronide + bilirubin
show the reaction diagram
-
-
-
-
?
bilirubin monoglucuronide + bilirubin monoglucuronide
bilirubin diglucuronide + bilirubin
show the reaction diagram
Rattus norvegicus Wistar
-
-
-
?
bilirubin monoglucuronide + bilirubin monoglucuronide
bilirubin diglucuronide + bilirubin
show the reaction diagram
Rattus norvegicus Wistar
-
-
-
-
?
serotonin + UDP-glucuronate
UDP + 3-(2-aminoethyl)-1H-indol-5-yl beta-D-glucuronide
show the reaction diagram
Q20CK6, Q20CK7, Q20CK8, Q20CK9, Q20CL0, Q20CL1, Q20CL2, Q20CL3, Q20CL4, Q20CL5, Q20CL6
-
-
-
?
UDP-glucuronate + 1-naphthol
UDP + beta-D-glucuronosyl-(1-naphthol)
show the reaction diagram
Q20CK6, Q20CK7, Q20CK8, Q20CK9, Q20CL0, Q20CL1, Q20CL2, Q20CL3, Q20CL4, Q20CL5, Q20CL6
-
-
-
?
UDP-glucuronate + 4-methylumbelliferone
UDP + beta-D-glucuronosyl-(4-methylumbelliferone)
show the reaction diagram
Q20CK6, Q20CK7, Q20CK8, Q20CK9, Q20CL0, Q20CL1, Q20CL2, Q20CL3, Q20CL4, Q20CL5, Q20CL6
-
-
-
?
UDP-glucuronate + 4-nitrophenol
UDP + 4-nitrophenol beta-D-glucuronide
show the reaction diagram
Q20CK6, Q20CK7, Q20CK8, Q20CK9, Q20CL0, Q20CL1, Q20CL2, Q20CL3, Q20CL4, Q20CL5, Q20CL6
-
-
-
?
UDP-glucuronate + buprenorphine
UDP + buprenorphine glucuronide
show the reaction diagram
Q20CK6, Q20CK7, Q20CK8, Q20CK9, Q20CL0, Q20CL1, Q20CL2, Q20CL3, Q20CL4, Q20CL5, Q20CL6
-
-
-
?
UDP-glucuronic acid + bilirubin
bilirubin glucuronoside + UDP
show the reaction diagram
-
-
-
-
?
UDP-glucuronic acid + bilirubin
bilirubin glucuronoside + UDP
show the reaction diagram
P22309
-
-
-
?
UDP-glucuronic acid + bilirubin
bilirubin glucuronoside + UDP
show the reaction diagram
Q20CK6, Q20CK7, Q20CK8, Q20CK9, Q20CL0, Q20CL1, Q20CL2, Q20CL3, Q20CL4, Q20CL5, Q20CL6
-
-
-
?
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
-
-
-
-
?
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
-
-
-
-
?
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Mg2+
-
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
1-Naphthol
-
-
4-hydroxyphenytoin
-
-
-
4-Methylumbelliferone
-
-
7-ethyl-10-hydroxycamptothecin
-
weak inhibitor of bilirubin glucuronidation
anthraflavic acid
-
-
baicalein
-
-
carvedilol
-
-
daidzein
-
-
ethinylestradiol
-
-
Farnesol
-
-
ketoconazole
-
-
levothyroxine
-
-
-
niflumic acid
-
-
raltegravir
-
-
-
riluzole
-
-
-
ritonavir
-
-
SN-38
-
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.02
bilirubin
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.033
bilirubin monoglucuronide
-
-
0.035
bilirubin monoglucuronide
-
-
additional information
additional information
-
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)
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.24
1-Naphthol
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.12
4-hydroxyphenytoin
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
-
0.1
4-Methylumbelliferone
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.3564
7-ethyl-10-hydroxycamptothecin
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.0036
anthraflavic acid
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.007
baicalein
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.027
carvedilol
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.0073
daidzein
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.021
ethinylestradiol
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.047
Farnesol
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.027
ketoconazole
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.0049
levothyroxine
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
-
0.053
niflumic acid
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.17
raltegravir
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
-
0.18
riluzole
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
-
0.003
ritonavir
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
0.36
SN-38
-
in 100 mM Tris-HCl buffer (pH 7.4) with 5 mM MgCl2, at 37C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4
Q20CK6, Q20CK7, Q20CK8, Q20CK9, Q20CL0, Q20CL1, Q20CL2, Q20CL3, Q20CL4, Q20CL5, Q20CL6
assay at; assay at; assay at; assay at; assay at; assay at; assay at; assay at; assay at; assay at; assay at
7.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
Q20CK6, Q20CK7, Q20CK8, Q20CK9, Q20CL0, Q20CL1, Q20CL2, Q20CL3, Q20CL4, Q20CL5, Q20CL6
assay at; assay at; assay at; assay at; assay at; assay at; assay at; assay at; assay at; assay at; assay at
37
-
assay at
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
Rattus norvegicus Wistar
-
-
-
-
Manually annotated by BRENDA team
Rattus norvegicus Wistar
-
-
-
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
50000
-
SDS-PAGE, each UGT1A isoform shows a single band at 50 to 55 kDa, owing to the differences in the levels of glycosylation
692032
160000
-
gel filtration
489619, 489620
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
-
x * 28000, SDS-PAGE
?
Rattus norvegicus Wistar
-
x * 28000, SDS-PAGE
-
monomer
P22309
-
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
following incubation of solubilized plasma membrane with pronase at 37C for 180 min, 80% of enzyme activity is lost
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
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; expressed in HEK293 cells
Q20CK6, Q20CK7, Q20CK8, Q20CK9, Q20CL0, Q20CL1, Q20CL2, Q20CL3, Q20CL4, Q20CL5, Q20CL6
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
F83L
-
the mutant exhibits less than 5% of wild type conjugation capacity
G211A
-
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
-
the mutant exhibits about 30% of wild type conjugation capacity
N400D
-
the mutant exhibits about 60% of wild type conjugation capacity
R336L
-
the mutant exhibits about 80% of wild type conjugation capacity
T3279G
-
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
-
the mutant exhibits less than 5% of wild type conjugation capacity
I294T
-
the mutant exhibits about 40% of wild type conjugation capacity
additional information
-
an increased number of TA repeats in the promoter region of the gene is associated with hyperbilirubinemia and in sickle cell disease patients, and the frequency for subsequent complications (cholelithiasis and cholecystectomy) is increased
additional information
-
subtype *28, A(TA)6TAA changed to A(TA)7TAA at nucleotide 53, diplotypes of this subtype plus the T3279G subtype (*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 and wild-type/*60 + wild-type/*28 + wild-type/*6) are significantly related to hyperbilirubinemia development, also *60/*60 + wild-type/*28
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
-
an increased level of TA repeats in the promoter of the gene is associated with a higher bilirubinemia in sickle cell disease patients (young, Bantu beta S haplotype), the development of cholelithiasis and cholecystectomy are more frequent in groups with higher TA repeats, no influence of alpha thalassaemia
medicine
-
the T3279G gene variant is associated with the development of hyperbilirubinemia, no gender difference between genetic subtypes