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Literature summary extracted from

  • Qu, Q.; Sharom, F.J.
    Proximity of bound Hoechst 33342 to the ATPase catalytic sites places the drug binding site of P-glycoprotein within the cytoplasmic membrane leaflet (2002), Biochemistry, 41, 4744-4752.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 orthovanadate rapid and complete inhibition in the presence of ATP and Co2+, very stable Pgp-ADP-Vi-Co2+ complex Cricetulus griseus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
7.6.2.2 plasma membrane transmembrane protein, location in the membrane Cricetulus griseus 5886
-

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 Cricetulus griseus the Pgp multidrug transporter carries out ATP-driven cellular efflux of a wide variety of hydrophobic drugs, natural products and peptides ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
7.6.2.2 Cricetulus griseus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
7.6.2.2
-
 Cricetulus griseus

Reaction

EC Number Reaction Comment Organism Reaction ID
7.6.2.2 ATP + H2O + xenobiotic[side 1] = ADP + phosphate + xenobiotic[side 2] mechanism Cricetulus griseus
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
7.6.2.2 CHRB30 cell Chinese hamster ovary cells Cricetulus griseus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in Hoechst 33342 binding site, proximity of bound Hoechst 33342 to the ATPase catalytic sites places the drug binding site of P-glycoprotein within the cytoplasmic membrane leaflet, Cys-428 and Cys-1071 are within the catalytic sites of Pgp, one within each of the Walker A motifs of the nucleotide binding folds, mechanism Cricetulus griseus ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
-
 ?
7.6.2.2 additional information the Pgp multidrug transporter carries out ATP-driven cellular efflux of a wide variety of hydrophobic drugs, natural products and peptides Cricetulus griseus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 MDR
-
 Cricetulus griseus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
7.6.2.2 37
-
 assay at Cricetulus griseus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
7.6.2.2 7.5
-
 assay at Cricetulus griseus