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Literature summary for 7.6.2.2 extracted from

  • Lagas, J.S.; van der Kruijssen, C.M.; van de Wetering, K.; Beijnen, J.H.; Schinkel, A.H.
    Transport of diclofenac by breast cancer resistance protein (ABCG2) and stimulation of multidrug resistance protein 2 (ABCC2)-mediated drug transport by diclofenac and benzbromarone (2009), Drug Metab. Dispos., 37, 129-136.
    View publication on PubMed
Search for more literature for 7.6.2.2

Activating Compound

Activating Compound Comment Organism Structure
benzbromarone MRP2-mediated transport of amphipathic lipophilic drugs Homo sapiens
diclofenac MRP2-mediated transport of amphipathic lipophilic drugs, stimulates paclitaxel, docetaxel, and saquinavir transport Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
enzyme expression in MDCK II cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
benzbromarone
-
 Homo sapiens
diclofenac inhibits MRP2-mediated drug transport Homo sapiens
elacridar inhibits P-gp Canis lupus familiaris
additional information inhibition kinetics, overview Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
 Homo sapiens 16020
-
membrane
-
 Canis lupus familiaris 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 + methotrexate/in Canis lupus familiaris
-
 ADP + phosphate + methotrexate/out
-
 ?
ATP + H2O + xenobiotic/in Homo sapiens
-
 ADP + phosphate + xenobiotic/out
-
 ?
ATP + H2O + xenobiotic/in Canis lupus familiaris
-
 ADP + phosphate + xenobiotic/out
-
 ?
additional information Homo sapiens stimulation of elimination via MRP2 may result in suboptimal chemotherapeutic drug concentrations, and stimulation of MRP2 activity in tumors may lead to increased efflux of chemotherapeutic drugs and thereby drug resistance ?
-
 ?

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris
-
-
-
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
MDCK II cell
-
 Canis lupus familiaris
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + diclofenac/in substrate of BCRP, but not of P-gp and MDR1 Homo sapiens ADP + phosphate + diclofenac/out
-
 ?
ATP + H2O + docetaxel/in
-
 Homo sapiens ADP + phosphate + docetaxel/out
-
 ?
ATP + H2O + methotrexate/in
-
 Homo sapiens ADP + phosphate + methotrexate/out
-
 ?
ATP + H2O + methotrexate/in
-
 Canis lupus familiaris ADP + phosphate + methotrexate/out
-
 ?
ATP + H2O + paclitaxel/in
-
 Homo sapiens ADP + phosphate + paclitaxel/out
-
 ?
ATP + H2O + saquinavir/in
-
 Homo sapiens ADP + phosphate + saquinavir/out
-
 ?
ATP + H2O + xenobiotic/in
-
 Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?
ATP + H2O + xenobiotic/in
-
 Canis lupus familiaris ADP + phosphate + xenobiotic/out
-
 ?
additional information stimulation of elimination via MRP2 may result in suboptimal chemotherapeutic drug concentrations, and stimulation of MRP2 activity in tumors may lead to increased efflux of chemotherapeutic drugs and thereby drug resistance Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
ABCB1
-
 Homo sapiens
ABCC2
-
 Homo sapiens
ABCG2
-
 Homo sapiens
BCRP
-
 Homo sapiens
breast cancer resistance protein
-
 Homo sapiens
MDR1
-
 Homo sapiens
MRP2
-
 Homo sapiens
MRP2
-
 Canis lupus familiaris
multidrug resistance protein 2
-
 Homo sapiens
P-glycoprotein
-
 Homo sapiens
P-gp
-
 Homo sapiens
P-gp
-
 Canis lupus familiaris

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
5.5 7.4 assay at pH 5.5 or pH 7.4 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens
ATP
-
 Canis lupus familiaris