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Literature summary for 7.6.2.2 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
Search for more literature for 7.6.2.2

Activating Compound

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

Inhibitors

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

KM Value [mM]

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

Localization

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

Organism

Organism UniProt Comment Textmining
Cricetulus griseus
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein
-
 Cricetulus griseus

Source Tissue

Source Tissue Comment Organism Textmining
CHRB30 cell
-
 Cricetulus griseus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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
-
 ?
additional information the P-glycoprotein contains two distinct sites for drug binding and transport, these sites interact in a positively cooperative manner Cricetulus griseus ?
-
 ?
rhodamine 123/in + ATP + H2O
-
 Cricetulus griseus rhodamine 123/out + ADP + phosphate
-
 ?