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Literature summary extracted from

  • Paul, S.; Breuninger, L.M.; Kruh, G.D.
    ATP-dependent transport of lipophilic cytotoxic drugs by membrane vesicles prepared from MRP-overexpressing HL60/ADR cells (1996), Biochemistry, 35, 14003-14011.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 arsenate competitive inhibitor of daunorubicin transport Homo sapiens
7.6.2.2 azidophenacylglutathione competitive inhibitor of daunorubicin transport Homo sapiens
7.6.2.2 cyclosporin A weak competitive inhibitor of daunorubicin transport Homo sapiens
7.6.2.2 genistein competitive inhibitor of daunorubicin transport Homo sapiens
7.6.2.2 GSH competitive inhibitor of daunorubicin transport Homo sapiens
7.6.2.2 GSSG competitive inhibitor of daunorubicin transport Homo sapiens
7.6.2.2 MK571 competitive inhibitor of daunorubicin transport Homo sapiens
7.6.2.2 PSC833 weak competitive inhibitor of daunorubicin transport Homo sapiens
7.6.2.2 verapamil weak competitive inhibitor of daunorubicin transport Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
7.6.2.2 0.0055
-
vincristine/in
-
Homo sapiens
7.6.2.2 0.0057
-
etoposide/in
-
Homo sapiens
7.6.2.2 0.0061
-
daunorubicin/in
-
Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
7.6.2.2 additional information Homo sapiens enzyme confers cellular resistance to a variety of natural product cytotoxic agents ?
-
?

Organism

EC Number Organism UniProt Comment Textmining
7.6.2.2 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
7.6.2.2 HEK-293 cell
-
Homo sapiens
-
7.6.2.2 HL-60 cell MRP-overexpressing HL60/ADR cells Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 daunorubicin/in + ATP + H2O
-
Homo sapiens daunorubicin/out + ADP + phosphate
-
?
7.6.2.2 etoposide/in + ATP + H2O
-
Homo sapiens etoposide/out + ADP + phosphate
-
?
7.6.2.2 additional information enzyme confers cellular resistance to a variety of natural product cytotoxic agents Homo sapiens ?
-
?
7.6.2.2 vincristine/in + ATP + H2O
-
Homo sapiens vincristine/out + ADP + phosphate
-
?