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Literature summary for 7.6.2.2 extracted from

  • Conseil, G.; Rothnie, A.J.; Deeley, R.G.; Cole, S.P.
    Multiple roles of charged amino acids in cytoplasmic loop 7 for expression and function of the multidrug and organic anion transporter MRP1 (ABCC1) (2009), Mol. Pharmacol., 75, 397-406.
    View publication on PubMed
Search for more literature for 7.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type an dmutant enzymes in HEK-293 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
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
D1183E site-directed mutagenesis, the mutant shows transport activities similar to the wild-type enzyme, but reduced expression level Homo sapiens
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
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
K1181A site-directed mutagenesis, the mutant shows similar or higher expression level compared to the wild-type enzyme Homo sapiens
R1166K site-directed mutagenesis, the mutant shows transport activities similar to the wild-type enzyme, but reduced expression level Homo sapiens
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

Localization Comment Organism GeneOntology No. Textmining
membrane
-
 Homo sapiens 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + xenobiotic/in Homo sapiens
-
 ADP + phosphate + xenobiotic/out
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
 relative activities and substrate specificity of wild-type an dmutant enzymes Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
8-azido-ATP + H2O + xenobiotic/in
-
 Homo sapiens 8-azido-ADP + phosphate + xenobiotic/out
-
 ?
ATP + H2O + 17beta-estradiol 17-(beta-D-glucuronide)/in
-
 Homo sapiens ADP + phosphate + 17beta-estradiol 17-(beta-D-glucuronide)/out
-
 ?
ATP + H2O + estrone-3-sulfate/in
-
 Homo sapiens ADP + phosphate + estrone-3-sulfate/out
-
 ?
ATP + H2O + glutathione/in
-
 Homo sapiens ADP + phosphate + glutathione/out
-
 ?
ATP + H2O + leukotriene C4/in
-
 Homo sapiens ADP + phosphate + leukotriene C4/out
-
 ?
ATP + H2O + methotrexate/in
-
 Homo sapiens ADP + phosphate + methotrexate/out
-
 ?
ATP + H2O + xenobiotic/in
-
 Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?
ATP + H2O + xenobiotic/in ATP-dependent MRP1-mediated uptake of labeled substrates in membrane vesicles Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?

Synonyms

Synonyms Comment Organism
ABCC1
-
 Homo sapiens
MRP1
-
 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
7.5
-
 assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens