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Literature summary for 7.6.2.2 extracted from

  • van de Wetering, K.; Burkon, A.; Feddema, W.; Bot, A.; de Jonge, H.; Somoza, V.; Borst, P.
    Intestinal breast cancer resistance protein (BCRP)/Bcrp1 and multidrug resistance protein 3 (MRP3)/Mrp3 are involved in the pharmacokinetics of resveratrol (2009), Mol. Pharmacol., 75, 876-885.
    View publication on PubMed
Search for more literature for 7.6.2.2

Protein Variants

Protein Variants Comment Organism
additional information absence of Mrp3 in knockout mice results in altered disposition of resveratrol-3-glucuronide and its parent compound resveratrol, leading to a reduced percentage of resveratrol being excreted via the urine in Mrp3-/- mice. Knockout of BCRP in mice results in high plasma levels of resveratrol-di-sulfate, a resveratrol metabolite hardly detectable in the plasma of wild-type mice and in an increased disposal of resveratrol via the urine Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
resveratrol disulfate acts as a competitive inhibitor of BCRP-mediated methotrexate transport Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.005
-
 resveratrol-3-sulfate [side 1] pH 7.4, 37°C, recombinant BCRP Mus musculus
0.01
-
 resveratrol disulfate pH 7.4, 37°C, recombinant BCRP Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
 Mus musculus 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + xenobiotic/in Mus musculus
-
 ADP + phosphate + xenobiotic/out
-
 ?

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
enterocyte Mrp3 is located in the basolateral, Bcrp1 in the apical membranes of enterocytes Mus musculus
-
intestine
-
 Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + resveratrol disulfate/in substrate of BCRP in vitro Mus musculus ADP + phosphate + resveratrol disulfate/out
-
 ?
ATP + H2O + resveratrol-3-glucuronide/in substrate of Mrp3 and BCRP in vitro as sulfate Mus musculus ADP + phosphate + resveratrol-3-glucuronide/out
-
 ?
ATP + H2O + resveratrol-3-sulfate [side 1]
-
 Mus musculus ADP + phosphate + resveratrol-3-sulfate [side 2]
-
 ?
ATP + H2O + resveratrol/in substrate of BCRP in vitro as sulfate Mus musculus ADP + phosphate + resveratrol/out
-
 ?
ATP + H2O + xenobiotic/in
-
 Mus musculus ADP + phosphate + xenobiotic/out
-
 ?

Synonyms

Synonyms Comment Organism
ABCC3
-
 Mus musculus
ABCG2
-
 Mus musculus
Bcrp1
-
 Mus musculus
breast cancer resistance protein
-
 Mus musculus
MRP3
-
 Mus musculus
multidrug resistance protein 3
-
 Mus musculus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Mus musculus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Mus musculus

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Mus musculus

General Information

General Information Comment Organism
physiological function absence of Mrp3 in knockout mice results in altered disposition of resveratrol-3-glucuronide and its parent compound resveratrol, leading to a reduced percentage of resveratrol being excreted via the urine in Mrp3-/- mice. Knockout of BCRP in mice results in high plasma levels of resveratrol-di-sulfate, a resveratrol metabolite hardly detectable in the plasma of wild-type mice and in an increased disposal of resveratrol via the urine Mus musculus