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Literature summary for 7.6.2.2 extracted from

  • Heikkinen, A.T.; Moenkkoenen, J.
    Protein concentration and pH affect the apparent P-glycoprotein-ATPase activation kinetics (2008), Int. J. Pharm., 346, 169-172.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
monensin protein concentration of enzyme is inversely related to the maximum activation of ATPase activity achieved Homo sapiens
quinidine protein concentration of enzyme is inversely related to the maximum activation of ATPase activity achieved Homo sapiens
verapamil protein concentration of enzyme is inversely related to the maximum activation of ATPase activity achieved Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression in insect cell Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Homo sapiens 16020
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isoform MDR1
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + monensin/in affinity of verapamil to MDR1 is not affected by pH value. Protein concentration is inversely related to the maximum activation of ATPase activity achieved Homo sapiens ADP + phosphate + monensin/out
-
?
ATP + H2O + quinidine/in affinity of qunidine to MDR1 is higher at pH 7.4 than at pH 6.8. Protein concentration is inversely related to the maximum activation of ATPase activity achieved Homo sapiens ADP + phosphate + quinidine/out
-
?
ATP + H2O + verapamil/in
-
Homo sapiens ADP + phosphate + verapamil/out affinity of verapamil to MDR1 is higher at pH 7.4 than at pH 6.8. Protein concentration is inversely related to the maximum activation of ATPase activity achieved ?