EC Number | Activating Compound | Comment | Organism | Structure |
---|---|---|---|---|
7.6.2.2 | campesterol | enhances paclitaxel-stimulated ATPase activity of enzyme | Homo sapiens | |
7.6.2.2 | cholesterol | presence of cholesterol in liposomes increases the binding affinity of small drug substrates with molecular masses below 500 Da, does not affect that of drugs with molecular mass of between 800 and 900 Da, and suppresses that of valinomycin with a molecular mass greater than 1000. Cholesterol enhances paclitaxel-stimulated ATPase activity of enzyme | Homo sapiens | |
7.6.2.2 | sitosterol | enhances paclitaxel-stimulated ATPase activity of enzyme | Homo sapiens | |
7.6.2.2 | stigmasterol | enhances paclitaxel-stimulated ATPase activity of enzyme | Homo sapiens |
EC Number | Cloned (Comment) | Organism |
---|---|---|
7.6.2.2 | expression in insect cells | Homo sapiens |
EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
7.6.2.2 | cholesterol | presence of cholesterol in liposomes increases the binding affinity of small drug substrates with molecular masses below 500 Da, does not affect that of drugs with molecular mass of between 800 and 900 Da, and suppresses that of valinomycin with a molecular mass greater than 1000 | Homo sapiens |
EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|---|
7.6.2.2 | 0.0009 | - |
ATP | pH 7.5, 37°C, paclitaxel-stimulated ATPase activity, presence of 20% ergosterol | Homo sapiens | |
7.6.2.2 | 0.001 | - |
ATP | pH 7.5, 37°C, paclitaxel-stimulated ATPase activity, presence of 20% campesterol | Homo sapiens | |
7.6.2.2 | 0.001 | - |
nicardipine/in | pH 7.5, 37°C, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0011 | - |
ATP | pH 7.5, 37°C, paclitaxel-stimulated ATPase activity, presence of 20% sitosterol | Homo sapiens | |
7.6.2.2 | 0.0013 | - |
paclitaxel | pH 7.5, 37°C, presence of 5% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0013 | - |
vinblastine/in | pH 7.5, 37°C, presence of 5% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0014 | - |
paclitaxel | pH 7.5, 37°C | Homo sapiens | |
7.6.2.2 | 0.0014 | - |
ATP | pH 7.5, 37°C, paclitaxel-stimulated ATPase activity | Homo sapiens | |
7.6.2.2 | 0.0014 | - |
ATP | pH 7.5, 37°C, paclitaxel-stimulated ATPase activity, presence of 20% stigmasterol | Homo sapiens | |
7.6.2.2 | 0.0015 | - |
nicardipine/in | pH 7.5, 37°C, presence of 5% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0016 | - |
ATP | pH 7.5, 37°C, paclitaxel-stimulated ATPase activity, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0016 | - |
paclitaxel | pH 7.5, 37°C, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0016 | - |
vinblastine/in | pH 7.5, 37°C, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0017 | - |
vinblastine/in | pH 7.5, 37°C | Homo sapiens | |
7.6.2.2 | 0.0022 | - |
verapamil | pH 7.5, 37°C, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0022 | - |
valinomycin/in | pH 7.5, 37°C, presence of 5% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0025 | - |
valinomycin/in | pH 7.5, 37°C | Homo sapiens | |
7.6.2.2 | 0.0026 | - |
nicardipine/in | pH 7.5, 37°C | Homo sapiens | |
7.6.2.2 | 0.0027 | - |
vincristine | pH 7.5, 37°C, presence of 5% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0035 | - |
valinomycin/in | pH 7.5, 37°C, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0037 | - |
vincristine | pH 7.5, 37°C | Homo sapiens | |
7.6.2.2 | 0.0038 | - |
verapamil | pH 7.5, 37°C, presence of 5% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0039 | - |
vincristine | pH 7.5, 37°C, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.0041 | - |
verapamil | pH 7.5, 37°C | Homo sapiens | |
7.6.2.2 | 0.007 | - |
rhodamine B | pH 7.5, 37°C, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.009 | - |
rhodamine B | pH 7.5, 37°C, presence of 5% cholesterol | Homo sapiens | |
7.6.2.2 | 0.01 | - |
rhodamine 123 | pH 7.5, 37°C, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.014 | - |
rhodamine B | pH 7.5, 37°C | Homo sapiens | |
7.6.2.2 | 0.016 | - |
rhodamine 123 | pH 7.5, 37°C, presence of 5% cholesterol | Homo sapiens | |
7.6.2.2 | 0.021 | - |
rhodamine 123 | pH 7.5, 37°C | Homo sapiens | |
7.6.2.2 | 0.076 | - |
digoxin | pH 7.5, 37°C, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.12 | - |
digoxin | pH 7.5, 37°C, presence of 5% cholesterol | Homo sapiens | |
7.6.2.2 | 0.181 | - |
digoxin | pH 7.5, 37°C | Homo sapiens | |
7.6.2.2 | 0.394 | - |
dexamethasone | pH 7.5, 37°C, presence of 20% cholesterol | Homo sapiens | |
7.6.2.2 | 0.527 | - |
dexamethasone | pH 7.5, 37°C, presence of 5% cholesterol | Homo sapiens | |
7.6.2.2 | 0.826 | - |
dexamethasone | pH 7.5, 37°C | Homo sapiens |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
7.6.2.2 | additional information | Homo sapiens | the drug substrate binding site of isoform MDR1/P-glycoprotein may best fit to drugs with a molecular mass of between 800 and 900 Da, and cholesterol may support the recognition of smaller drugs by adjusting the drug-binding site | ? | - |
? |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
7.6.2.2 | Homo sapiens | - |
isoform MDR1/P-glycoprotein | - |
EC Number | Purification (Comment) | Organism |
---|---|---|
7.6.2.2 | recombinant protein, reconstitution in proteoliposomes containing varying concentrations of cholesterol | Homo sapiens |
EC Number | Renatured (Comment) | Organism |
---|---|---|
7.6.2.2 | reconstitution of purified recombinant protein in proteoliposomes containing varying concentrations of cholesterol | Homo sapiens |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
7.6.2.2 | ATP + H2O | - |
Homo sapiens | ADP + phosphate | - |
? | |
7.6.2.2 | ATP + H2O + nicardipine/in | - |
Homo sapiens | ADP + phosphate + nicardipine/out | - |
? | |
7.6.2.2 | ATP + H2O + valinomycin/in | - |
Homo sapiens | ADP + phosphate + valinomycin/out | - |
? | |
7.6.2.2 | ATP + H2O + vinblastine/in | - |
Homo sapiens | ADP + phosphate + vinblastine/out | - |
? | |
7.6.2.2 | dexamethasone/in + ATP + H2O | - |
Homo sapiens | dexamethasone/out + ADP + phosphate | - |
? | |
7.6.2.2 | digoxin/in + ATP + H2O | - |
Homo sapiens | digoxin/out + ADP + phosphate | - |
? | |
7.6.2.2 | additional information | the drug substrate binding site of isoform MDR1/P-glycoprotein may best fit to drugs with a molecular mass of between 800 and 900 Da, and cholesterol may support the recognition of smaller drugs by adjusting the drug-binding site | Homo sapiens | ? | - |
? | |
7.6.2.2 | nicardipine/in + ATP + H2O | - |
Homo sapiens | nicardipine/out + ADP + phosphate | - |
? | |
7.6.2.2 | paclitaxel/in + ATP + H2O | - |
Homo sapiens | paclitaxel/out + ADP + phosphate | - |
? | |
7.6.2.2 | rhodamine 123/in + ATP + H2O | - |
Homo sapiens | rhodamine 123/out + ADP + phosphate | - |
? | |
7.6.2.2 | rhodamine B/in + ATP + H2O | - |
Homo sapiens | rhodamine B/out + ADP + phosphate | - |
? | |
7.6.2.2 | valinomycin/in + ATP + H2O | - |
Homo sapiens | valinomycin/out + ADP + phosphate | - |
? | |
7.6.2.2 | verapamil/in + ATP + H2O | - |
Homo sapiens | verapamil/out + ADP + phosphate | - |
? | |
7.6.2.2 | vinblastine/in + ATP + H2O | - |
Homo sapiens | vinblastine/out + ADP + phosphate | - |
? | |
7.6.2.2 | vincristine/in + ATP + H2O | - |
Homo sapiens | vincristine/out + ADP + phosphate | - |
? |