BRENDA - Enzyme Database show

Multiple roles of charged amino acids in cytoplasmic loop 7 for expression and function of the multidrug and organic anion transporter MRP1 (ABCC1)

Conseil, G.; Rothnie, A.J.; Deeley, R.G.; Cole, S.P.; Mol. Pharmacol. 75, 397-406 (2009)

Data extracted from this reference:

Cloned(Commentary)
EC Number
Commentary
Organism
7.6.2.2
expression of wild-type an dmutant enzymes in HEK-293 cells
Homo sapiens
Engineering
EC Number
Amino acid exchange
Commentary
Organism
7.6.2.2
D1179A
site-directed mutagenesis, the mutant shows similar or higher expression level, but about 35% reduced drug transport activity and altered substrate specificity compared to the wild-type enzyme
Homo sapiens
7.6.2.2
D1183E
site-directed mutagenesis, the mutant shows transport activities similar to the wild-type enzyme, but reduced expression level
Homo sapiens
7.6.2.2
E1144A
site-directed mutagenesis, the mutant shows similar or higher expression level, but about 50% reduced drug transport activity compared to the wild-type enzyme
Homo sapiens
7.6.2.2
E1184A
site-directed mutagenesis, the mutant shows similar or higher expression level, but reduced activity and altered substrate specificity compared to the wild-type enzyme
Homo sapiens
7.6.2.2
K1181A
site-directed mutagenesis, the mutant shows similar or higher expression level compared to the wild-type enzyme
Homo sapiens
7.6.2.2
R1166K
site-directed mutagenesis, the mutant shows transport activities similar to the wild-type enzyme, but reduced expression level
Homo sapiens
7.6.2.2
R1173A
site-directed mutagenesis, the mutant shows similar or higher expression level, but increased activity and altered substrate specificity compared to the wild-type enzyme
Homo sapiens
Localization
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
7.6.2.2
membrane
-
Homo sapiens
16020
-
Metals/Ions
EC Number
Metals/Ions
Commentary
Organism
Structure
7.6.2.2
Mg2+
-
Homo sapiens
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
7.6.2.2
ATP + H2O + xenobiotic/in
Homo sapiens
-
ADP + phosphate + xenobiotic/out
-
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
7.6.2.2
Homo sapiens
-
-
-
Specific Activity [micromol/min/mg]
EC Number
Specific Activity Minimum [µmol/min/mg]
Specific Activity Maximum [µmol/min/mg]
Commentary
Organism
7.6.2.2
additional information
-
relative activities and substrate specificity of wild-type an dmutant enzymes
Homo sapiens
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
7.6.2.2
8-azido-ATP + H2O + xenobiotic/in
-
700297
Homo sapiens
8-azido-ADP + phosphate + xenobiotic/out
-
-
-
?
7.6.2.2
ATP + H2O + 17beta-estradiol 17-(beta-D-glucuronide)/in
-
700297
Homo sapiens
ADP + phosphate + 17beta-estradiol 17-(beta-D-glucuronide)/out
-
-
-
?
7.6.2.2
ATP + H2O + estrone-3-sulfate/in
-
700297
Homo sapiens
ADP + phosphate + estrone-3-sulfate/out
-
-
-
?
7.6.2.2
ATP + H2O + glutathione/in
-
700297
Homo sapiens
ADP + phosphate + glutathione/out
-
-
-
?
7.6.2.2
ATP + H2O + leukotriene C4/in
-
700297
Homo sapiens
ADP + phosphate + leukotriene C4/out
-
-
-
?
7.6.2.2
ATP + H2O + methotrexate/in
-
700297
Homo sapiens
ADP + phosphate + methotrexate/out
-
-
-
?
7.6.2.2
ATP + H2O + xenobiotic/in
-
700297
Homo sapiens
ADP + phosphate + xenobiotic/out
-
-
-
?
7.6.2.2
ATP + H2O + xenobiotic/in
ATP-dependent MRP1-mediated uptake of labeled substrates in membrane vesicles
700297
Homo sapiens
ADP + phosphate + xenobiotic/out
-
-
-
?
Temperature Optimum [°C]
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
7.6.2.2
37
-
assay at
Homo sapiens
pH Optimum
EC Number
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
7.6.2.2
7.5
-
assay at
Homo sapiens
Cofactor
EC Number
Cofactor
Commentary
Organism
Structure
7.6.2.2
ATP
-
Homo sapiens
Cloned(Commentary) (protein specific)
EC Number
Commentary
Organism
7.6.2.2
expression of wild-type an dmutant enzymes in HEK-293 cells
Homo sapiens
Cofactor (protein specific)
EC Number
Cofactor
Commentary
Organism
Structure
7.6.2.2
ATP
-
Homo sapiens
Engineering (protein specific)
EC Number
Amino acid exchange
Commentary
Organism
7.6.2.2
D1179A
site-directed mutagenesis, the mutant shows similar or higher expression level, but about 35% reduced drug transport activity and altered substrate specificity compared to the wild-type enzyme
Homo sapiens
7.6.2.2
D1183E
site-directed mutagenesis, the mutant shows transport activities similar to the wild-type enzyme, but reduced expression level
Homo sapiens
7.6.2.2
E1144A
site-directed mutagenesis, the mutant shows similar or higher expression level, but about 50% reduced drug transport activity compared to the wild-type enzyme
Homo sapiens
7.6.2.2
E1184A
site-directed mutagenesis, the mutant shows similar or higher expression level, but reduced activity and altered substrate specificity compared to the wild-type enzyme
Homo sapiens
7.6.2.2
K1181A
site-directed mutagenesis, the mutant shows similar or higher expression level compared to the wild-type enzyme
Homo sapiens
7.6.2.2
R1166K
site-directed mutagenesis, the mutant shows transport activities similar to the wild-type enzyme, but reduced expression level
Homo sapiens
7.6.2.2
R1173A
site-directed mutagenesis, the mutant shows similar or higher expression level, but increased activity and altered substrate specificity compared to the wild-type enzyme
Homo sapiens
Localization (protein specific)
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
7.6.2.2
membrane
-
Homo sapiens
16020
-
Metals/Ions (protein specific)
EC Number
Metals/Ions
Commentary
Organism
Structure
7.6.2.2
Mg2+
-
Homo sapiens
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
7.6.2.2
ATP + H2O + xenobiotic/in
Homo sapiens
-
ADP + phosphate + xenobiotic/out
-
-
?
Specific Activity [micromol/min/mg] (protein specific)
EC Number
Specific Activity Minimum [µmol/min/mg]
Specific Activity Maximum [µmol/min/mg]
Commentary
Organism
7.6.2.2
additional information
-
relative activities and substrate specificity of wild-type an dmutant enzymes
Homo sapiens
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
7.6.2.2
8-azido-ATP + H2O + xenobiotic/in
-
700297
Homo sapiens
8-azido-ADP + phosphate + xenobiotic/out
-
-
-
?
7.6.2.2
ATP + H2O + 17beta-estradiol 17-(beta-D-glucuronide)/in
-
700297
Homo sapiens
ADP + phosphate + 17beta-estradiol 17-(beta-D-glucuronide)/out
-
-
-
?
7.6.2.2
ATP + H2O + estrone-3-sulfate/in
-
700297
Homo sapiens
ADP + phosphate + estrone-3-sulfate/out
-
-
-
?
7.6.2.2
ATP + H2O + glutathione/in
-
700297
Homo sapiens
ADP + phosphate + glutathione/out
-
-
-
?
7.6.2.2
ATP + H2O + leukotriene C4/in
-
700297
Homo sapiens
ADP + phosphate + leukotriene C4/out
-
-
-
?
7.6.2.2
ATP + H2O + methotrexate/in
-
700297
Homo sapiens
ADP + phosphate + methotrexate/out
-
-
-
?
7.6.2.2
ATP + H2O + xenobiotic/in
-
700297
Homo sapiens
ADP + phosphate + xenobiotic/out
-
-
-
?
7.6.2.2
ATP + H2O + xenobiotic/in
ATP-dependent MRP1-mediated uptake of labeled substrates in membrane vesicles
700297
Homo sapiens
ADP + phosphate + xenobiotic/out
-
-
-
?
Temperature Optimum [°C] (protein specific)
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
7.6.2.2
37
-
assay at
Homo sapiens
pH Optimum (protein specific)
EC Number
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
7.6.2.2
7.5
-
assay at
Homo sapiens