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Literature summary for 7.6.2.2 extracted from

  • Shirasaka, Y.; Onishi, Y.; Sakurai, A.; Nakagawa, H.; Ishikawa, T.; Yamashita, S.
    Evaluation of human P-glycoprotein (MDR1/ABCB1) ATPase activity assay method by comparing with in vitro transport measurements: Michaelis-Menten kinetic analysis to estimate the affinity of P-glycoprotein to drugs (2006), Biol. Pharm. Bull., 29, 2465-2471.
    View publication on PubMed

Application

Application Comment Organism
analysis evaluation of high-speed ATPase activity assay method by comparing with in vitro transport assay systems using MDR1-transfected MDR1-MDCK cells. The kinetic parameters obtained in ATPase activity assay are not necessarily corresponding with those in in vitro transport assay. The combination of the ATPase activity assay and in vitro transport technologies gives insight into mechanisms Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression in Sf9 cell Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00576
-
vinblastine/in pH 6.8, 37°C Homo sapiens
0.00788
-
quinidine pH 6.8, 37°C Homo sapiens
0.0115
-
verapamil pH 6.8, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + quinidine/in EC50 value 0.0164 mM Homo sapiens ADP + phosphate + quinidine/out
-
?
ATP + H2O + verapamil/in
-
Homo sapiens ADP + phosphate + verapamil/out EC50 value 0.00285 mM ?
ATP + H2O + vinblastine/in
-
Homo sapiens ADP + phosphate + vinblastine/out
-
?