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Literature summary extracted from

  • Shapiro, A.B.; Ling, V.
    Positively cooperative sites for drug transport by P-glycoprotein with distinct specificities (1997), Eur. J. Biochem., 250, 130-137.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
7.6.2.2 Colchicine stimulates transport of rhodamine 123 Cricetulus griseus
7.6.2.2 daunorubicin stimulates transport of Hoechst 33342 Cricetulus griseus
7.6.2.2 doxorubicin stimulates transport of Hoechst 33342 Cricetulus griseus
7.6.2.2 Hoechst 33342 stimulates transport of rhodamine 123 Cricetulus griseus
7.6.2.2 quercetin stimulates transport of rhodamine 123 Cricetulus griseus
7.6.2.2 rhodamine 123 stimulates transport of Hoechst 33342 Cricetulus griseus

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 actinomycin D inhibits transport of Hoechst 3343 and rhodamine 123 Cricetulus griseus
7.6.2.2 Colchicine inhibits transport of Hoechst 3342 Cricetulus griseus
7.6.2.2 daunorubicin inhibits transport of rhodamine 123 Cricetulus griseus
7.6.2.2 doxorubicin inhibits transport of rhodamine 123 Cricetulus griseus
7.6.2.2 etoposide inhibits transport of Hoechst 3343 and rhodamine 123 Cricetulus griseus
7.6.2.2 quercetin inhibits transport of Hoechst 33342 Cricetulus griseus
7.6.2.2 vinblastine inhibits transport of Hoechst 3343 and rhodamine 123 Cricetulus griseus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
7.6.2.2 0.0135
-
 rhodamine 123/in
-
 Cricetulus griseus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
7.6.2.2 plasma membrane
-
 Cricetulus griseus 5886
-

Organism

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

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
7.6.2.2 glycoprotein
-
 Cricetulus griseus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
7.6.2.2 CHRB30 cell
-
 Cricetulus griseus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 Hoechst 33342/in + ATP + H2O i.e. 2-[2-(4-ethoxyphenyl)-6-benzimidazolyl]-6-(1-methyl-4-piperazinyl)benzimidazole Cricetulus griseus Hoechst 33342/out + ADP + H2O
-
 ?
7.6.2.2 additional information the P-glycoprotein contains two distinct sites for drug binding and transport, these sites interact in a positively cooperative manner Cricetulus griseus ?
-
 ?
7.6.2.2 rhodamine 123/in + ATP + H2O
-
 Cricetulus griseus rhodamine 123/out + ADP + phosphate
-
 ?