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Literature summary for 7.6.2.3 extracted from

  • Renes, J.; De Vries, E.; Nienhuis, E.; Jansen, P.; Mueller, M.
    ATP- and glutathione-dependent transport of chemotherapeutic drugs by the multidrug resistance protein MRP1 (1999), Br. J. Pharmacol., 126, 681-688 .
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
glutathione
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
MK571
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
plasma membrane
-
Homo sapiens 5886
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + glutathione-S-conjugate[side 1] Homo sapiens
-
ADP + phosphate + glutathione-S-conjugate[side 2]
-
?
ATP + H2O + leukotriene C4[side 1] Homo sapiens
-
ADP + phosphate + leukotriene C4[side 2]
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P33527
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A2780AD cell
-
Homo sapiens
-
GLC-4/ADR cell
-
Homo sapiens
-
SW-1573 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + glutathione-S-conjugate[side 1]
-
Homo sapiens ADP + phosphate + glutathione-S-conjugate[side 2]
-
?
ATP + H2O + leukotriene C4[side 1]
-
Homo sapiens ADP + phosphate + leukotriene C4[side 2]
-
?
ATP + H2O + S-(daunorubicinyl)glutathione[side 1]
-
Homo sapiens ADP + phosphate + S-(daunorubicinyl)glutathione[side 2]
-
?
ATP + H2O + S-(vincristinyl)glutathione[side 1]
-
Homo sapiens ADP + phosphate + S-(vincristinyl)glutathione[side 2]
-
?
additional information the enzyme does not mediate transport of N-(4',4'-azo-n-pentyl)-21-deoxy-ajmalinium, vincristine and daunorubicin per se. N-(4',4'-azo-n-pentyl)-21-deoxy-ajmalinium is also not transported as S-glutathione conjugate Homo sapiens ?
-
?

Subunits

Subunits Comment Organism
? x * 180000, SDS-PAGE Homo sapiens

Synonyms

Synonyms Comment Organism
MRP1
-
Homo sapiens
multidrug resistance protein
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0004
-
with S-(daunorubicinyl)glutathione as substrate, at pH 7.4 and 37°C Homo sapiens MK571