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Literature summary for 7.6.2.2 extracted from

  • Eng, K.T.; Berdis, A.J.
    A novel non-natural nucleoside that influences P-glycoprotein activity and mediates drug resistance (2010), Biochemistry, 49, 1640-1648.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
N-(2'-deoxy-beta-D-ribofuranosyl)-5-cyclohexyl-1H-indole nontransported substrate of P-glycoprotein Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00006
-
N-(2'-deoxy-beta-D-ribofuranosyl)-5-cyclohexyl-1H-indole/in 37°C, pH not specified in the publication Homo sapiens
0.0002
-
vinblastine/in 37°C, pH not specified in the publication Homo sapiens
0.0004
-
cyclosporine A/in 37°C, pH not specified in the publication Homo sapiens
0.00085
-
doxorubicin/in 37°C, pH not specified in the publication Homo sapiens
0.0009
-
paclitaxel/in 37°C, pH not specified in the publication Homo sapiens
0.0031
-
calcein/in 37°C, pH not specified in the publication Homo sapiens
0.004
-
verapamil/in 37°C, pH not specified in the publication Homo sapiens
0.037
-
colchicine/in 37°C, pH not specified in the publication Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + calcein/in
-
Homo sapiens ADP + phosphate + calcein/out
-
?
ATP + H2O + colchicine/in
-
Homo sapiens ADP + phosphate + colchicine/out
-
?
ATP + H2O + cyclosporine A/in
-
Homo sapiens ADP + phosphate + cyclosporine A/out
-
?
ATP + H2O + doxorubicin/in
-
Homo sapiens ADP + phosphate + doxorubicin/out
-
?
ATP + H2O + N-(2'-deoxy-beta-D-ribofuranosyl)-5-cyclohexyl-1H-indole/in nontransported substrate of P-glycoprotein Homo sapiens ?
-
?
ATP + H2O + paclitaxel/in
-
Homo sapiens ADP + phosphate + paclitaxel/out
-
?
ATP + H2O + verapamil/in
-
Homo sapiens ADP + phosphate + verapamil/out
-
?
ATP + H2O + vinblastine/in
-
Homo sapiens ADP + phosphate + vinblastine/out
-
?