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Literature summary for 7.6.2.2 extracted from

  • Wesolowska, O.; Hendrich, A.B.; Laniapietrzak, B.; Wisniewski, J.; Molnar, J.; Ocsovszki, I.; Michalak, K.
    Perturbation of the lipid phase of a membrane is not involved in the modulation of MRP1 transport activity by flavonoids (2009), Cell. Mol. Biol. Lett., 14, 199-221.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 7.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
expression of the enzyme in L5178Y mouse T lymphoma parent cell line using the pHa MDR1/A retrovirus Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
acacetin
-
 Homo sapiens
apigenin
-
 Homo sapiens
indomethacin
-
 Homo sapiens
MK-571
-
 Homo sapiens
additional information flavonoids inhibit the MRP1-mediated efflux of fluorescent substrate both from human erythrocytes and MDA-MB-231 resistant breast cancer cells, enzyme molecular modeling, overview Homo sapiens
morin
-
 Homo sapiens
myricetin
-
 Homo sapiens
probenecid
-
 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
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
erythrocyte
-
 Homo sapiens
-
MDA-MB-231 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + 2',7'-bis-(3-carboxyethyl)-5-carboxyfluorescein/in fluorescent substrate Homo sapiens ADP + phosphate + 2',7'-bis-(3-carboxyethyl)-5-carboxyfluorescein/out
-
 ?
ATP + H2O + 2',7'-bis-(3-carboxyethyl)-6-carboxyfluorescein/in fluorescent substrate Homo sapiens ADP + phosphate + 2',7'-bis-(3-carboxyethyl)-6-carboxyfluorescein/out
-
 ?
ATP + H2O + rhodamine 123/in fluorescent substrate Homo sapiens ADP + phosphate + rhodamine 123/out
-
 ?
ATP + H2O + verapamil/in
-
 Homo sapiens ADP + phosphate + verapamil/out
-
 ?
ATP + H2O + xenobiotic/in
-
 Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?
additional information enzyme molecular modeling, overview Homo sapiens ?
-
 ?

Subunits

Subunits Comment Organism
More MRP1 is a 190-kDa protein composed of two hydrophobic transmembrane domains, each followed by a cytoplasmic nucleotide-binding domain Homo sapiens

Synonyms

Synonyms Comment Organism
MRP1
-
 Homo sapiens
multidrug resistanceassociated protein 1
-
 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

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information inhibition kinetics, overview Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0065
-
 pH 7.4, 37°C Homo sapiens acacetin
0.007
-
 pH 7.4, 37°C Homo sapiens morin
0.04
-
 pH 7.4, 37°C Homo sapiens apigenin
0.0526
-
 pH 7.4, 37°C Homo sapiens myricetin