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Literature summary for 7.6.2.2 extracted from

  • Szentpetery, Z.; Sarkadi, B.; Bakos, E.; Varadi, A.
    Functional studies on the MRP1 multidrug transporter: characterization of ABC-signature mutant variants (2004), Anticancer Res., 24, 449-456.
    View publication on PubMed
Search for more literature for 7.6.2.2

Application

Application Comment Organism
medicine MRP1 confers resistance to a wide variety of anticancer drugs Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
wild-type and mutant MRP1, expression in Sf9 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
G1433D mutation in the ABC-signature region of MRP1, mutant has negligible ATPase and vesicular transport activity, but shows normal ATP-binding, no transition state formation in the ATPase catalytic cycle Homo sapiens
G771D mutation in the ABC-signature region of MRP1, mutant has negligible ATPase and vesicular transport activity, but shows normal ATP-binding, no transition state formation in the ATPase catalytic cycle Homo sapiens
L1430R mutation in the ABC-signature region of MRP1, mutant has both ATPase and vesicular transport activity Homo sapiens
L768R mutation in the ABC-signature region of MRP1, mutant has both ATPase and vesicular transport activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
vanadate vanadate-sensitive ATPase activity Homo sapiens

Localization

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

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
160000
-
 x * 160000, recombinant, underglycosylated form of MRP1, SDS-PAGE Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + leukotriene C4/in Homo sapiens natural substrate of MRP1 ADP + phosphate + leukotriene C4/out
-
 ?
additional information Homo sapiens MRP1 is a key multidrug resistance ABC transporter in tumor cells ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + leukotriene C4/in natural substrate of MRP1 Homo sapiens ADP + phosphate + leukotriene C4/out
-
 ?
ATP + H2O + leukotriene C4/in natural substrate of MRP1, ATP-stimulated LTC4 uptake of Sf9 inside-out membrane vesicles, roles of the highly conserved ABC-signature regions in the two non-equivalent ABC units of MRP1, major functional role of the conserved glycine residues in both ABC units of MRP1 and formation of composite catalytically active sites involving both signature regions within the ABC domains Homo sapiens ADP + phosphate + leukotriene C4/out
-
 ?
ATP + H2O + N-ethylmaleimide S-glutathione/in roles of the highly conserved ABC-signature regions in the two non-equivalent ABC units of MRP1, major functional role of the conserved glycine residues in both ABC units of MRP1 and formation of composite catalytically active sites involving both signature regions within the ABC domains Homo sapiens ADP + phosphate + N-ethylmaleimide S-glutathione/out
-
 ?
additional information MRP1 is a key multidrug resistance ABC transporter in tumor cells Homo sapiens ?
-
 ?

Subunits

Subunits Comment Organism
? x * 160000, recombinant, underglycosylated form of MRP1, SDS-PAGE Homo sapiens

Synonyms

Synonyms Comment Organism
MRP1
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
23
-
 assay at, ATP-stimulated LTC4 uptake of inside-out vesicles Homo sapiens
37
-
 assay at, N-ethylmaleimide S-glutathione-stimulated ATPase activity Homo sapiens