Information on EC 3.6.3.44 - xenobiotic-transporting ATPase and Organism(s) Homo sapiens and UniProt Accession P08183

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Homo sapiens
UNIPROT: P08183
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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea


The taxonomic range for the selected organisms is: Homo sapiens

EC NUMBER
COMMENTARY hide
3.6.3.44
-
RECOMMENDED NAME
GeneOntology No.
xenobiotic-transporting ATPase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + H2O + xenobiotic/in = ADP + phosphate + xenobiotic/out
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of phosphoric ester
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-
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SYSTEMATIC NAME
IUBMB Comments
ATP phosphohydrolase (xenobiotic-exporting)
ABC-type (ATP-binding cassette-type) ATPase, characterized by the presence of two similar ATP-binding domains. Does not undergo phosphorylation during the transport process. The enzyme from Gram-positive bacteria and eukaryotic cells export a number of drugs, with unusual specificity, covering various groups of unrelated substances, while ignoring some that are closely related structurally. Several distinct enzymes may be present in a single eukaryotic cell. Many of them transport glutathione---drug conjugates. Some also show some 'flippase' (phospholipid-translocating ATPase; EC 3.6.3.1) activity.
CAS REGISTRY NUMBER
COMMENTARY hide
9000-83-3
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + H2O + C12E08/in
ADP + phosphate + C12E08/out
show the reaction diagram
-
-
-
?
ATP + H2O + daunorubicin/in
ADP + phosphate + daunorubicin/out
show the reaction diagram
-
-
-
?
ATP + H2O + diltiazem/in
ADP + phosphate + diltiazem/out
show the reaction diagram
-
-
-
?
ATP + H2O + Triton X-100/in
ADP + phosphate + Triton X-100/out
show the reaction diagram
above the critical micellar concentration, Triton X-100 leads to a rapid and irreversible decrease in extracellular acidification rate in both, wild-type and transfected cells which is due to cell lysis
-
-
?
ATP + H2O + Tween 80/in
ADP + phosphate + Tween 80/out
show the reaction diagram
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
show the reaction diagram
-
-
-
?
2,4-dinitrophenyl S-glutathione/in + ATP + H2O
2,4-dinitrophenyl S-glutathione/out + ADP + H2O
show the reaction diagram
-
-
-
?
6-mercaptopurine/in + ATP + H2O
6-mercaptopurine/out + ADP + phosphate
show the reaction diagram
-
-
-
?
8-azido-ATP + H2O + xenobiotic/in
8-azido-ADP + phosphate + xenobiotic/out
show the reaction diagram
-
-
-
-
?
9-(2-phosphonylmethoxyethyl)adenine/in + ATP + H2O
9-(2-phosphonylmethoxyethyl)adenine/out + ADP + phosphate
show the reaction diagram
-
-
-
?
aflatoxin B1-epoxide-GSH conjugate/in + ATP + H2O
aflatoxin B1-epoxide-GSH conjugate/out + ADP + phosphate
show the reaction diagram
-
-
-
?
aflatoxin B1/in + ATP + H2O
aflatoxin B1/out + ADP + phosphate
show the reaction diagram
ATP + H2O
?
show the reaction diagram
-
-
-
-
?
ATP + H2O
ADP + phosphate
show the reaction diagram
-
-
-
-
?
ATP + H2O + 1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane/in
ADP + phosphate + 1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 17beta-estradiol 17-(beta-D-glucuronide)/in
ADP + phosphate + 17beta-estradiol 17-(beta-D-glucuronide)/out
show the reaction diagram
ATP + H2O + 17beta-glucuronosyl oestradiol/in
ADP + phosphate + 17beta-glucuronosyl oestradiol/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 2',3'-dideoxycytidine/in
ADP + phosphate + 2',3'-dideoxycytidine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 2',7'-bis(carboxyethyl)-5(6)-carboxyfluorescein/in
ADP + phosphate + 2',7'-bis(carboxyethyl)-5(6)-carboxyfluorescein/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 2',7'-bis-(3-carboxyethyl)-5-carboxyfluorescein/in
ADP + phosphate + 2',7'-bis-(3-carboxyethyl)-5-carboxyfluorescein/out
show the reaction diagram
-
fluorescent substrate
-
-
?
ATP + H2O + 2',7'-bis-(3-carboxyethyl)-6-carboxyfluorescein/in
ADP + phosphate + 2',7'-bis-(3-carboxyethyl)-6-carboxyfluorescein/out
show the reaction diagram
-
fluorescent substrate
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
show the reaction diagram
-
Hoechst 33342
-
-
?
ATP + H2O + 2,5-dimethoxy-4-iodoamphetamine/in
ADP + phosphate + 2,5-dimethoxy-4-iodoamphetamine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 3,4-methylenedioxy-alpha-ethylphenethylamine/in
ADP + phosphate + 3,4-methylenedioxy-alpha-ethylphenethylamine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 4-(2-aminoethyl)benzenesulfonylfluoride/in
ADP + phosphate + 4-(2-aminoethyl)benzenesulfonylfluoride/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 4-aminohippuric acid/in
ADP + phosphate + 4-aminohippuric acid/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 5-(glutathione-S-yl)-N-methyl-alpha-methyldopamine/in
ADP + phosphate + 5-(glutathione-S-yl)-N-methyl-alpha-methyldopamine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 9-hydroxyrisperidone/in
ADP + phosphate + 9-hydroxyrisperidone/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + acitretin/in
ADP + phosphate + acitretin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + adefovir/in
ADP + phosphate + adefovir/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + allopurinol/in
ADP + phosphate + allopurinol/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + Bodipy-verapamil/in
ADP + phosphate + Bodipy-verapamil/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + buspirone/in
ADP + phosphate + buspirone/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + calcein acetoxymethylester/in
ADP + phosphate + calcein acetoxymethylester/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + calcein/in
ADP + phosphate + calcein/out
show the reaction diagram
ATP + H2O + cAMP/in
ADP + phosphate + cAMP/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cefazolin/in
ADP + phosphate + cefazolin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cefmetazole/in
ADP + phosphate + cefmetazole/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cefotaxime/in
ADP + phosphate + cefotaxime/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + ceftizoxime/in
ADP + phosphate + ceftizoxime/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + celecoxib/in
ADP + phosphate + celecoxib/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cGMP/in
ADP + phosphate + cGMP/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + chenodeoxycholylglycine/in
ADP + phosphate + chenodeoxycholylglycine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + chenodeoxycholyltaurine/in
ADP + phosphate + chenodeoxycholyltaurine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + chlorpromazine/in
ADP + phosphate + chlorpromazine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cholate/in
ADP + phosphate + cholate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cholesterol/in
ADP + phosphate + cholesterol/out
show the reaction diagram
ATP + H2O + cholylglycine/in
ADP + phosphate + cholylglycine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cholytaurine/in
ADP + phosphate + cholytaurine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + citalopram/in
ADP + phosphate + citalopram/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + colchicine/in
ADP + phosphate + colchicine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cyclic guanosine monophosphate/in
ADP + phosphate + cyclic guanosine monophosphate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cyclobenzaprine/in
ADP + phosphate + cyclobenzaprine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cyclosporin A/in
ADP + phosphate + cyclosporin A/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cyclosporine A/in
ADP + phosphate + cyclosporine A/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cytarabine/in
ADP + phosphate + cytarabine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + daunomycin/in
ADP + phosphate + daunomycin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + daunorubicin/in
ADP + phosphate + daunorubicin/out
show the reaction diagram
ATP + H2O + dehydroepiandrosterone sulfate/in
ADP + phosphate + dehydroepiandrosterone sulfate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + dehydroepiandrosterone-3-sulfate/in
ADP + phosphate + dehydroepiandrosterone-3-sulfate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + deoxycholylglycine/in
ADP + phosphate + deoxycholylglycine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + diazepam/in
ADP + phosphate + diazepam/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + diclofenac/in
ADP + phosphate + diclofenac/out
show the reaction diagram
-
substrate of BCRP, but not of P-gp and MDR1
-
-
?
ATP + H2O + digoxin/in
ADP + phosphate + digoxin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + diltiazem/in
ADP + phosphate + diltiazem/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + dipyridamole/in
ADP + phosphate + dipyridamole/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + docetaxel/in
ADP + phosphate + docetaxel/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + doxorubicin/in
ADP + phosphate + doxorubicin/out
show the reaction diagram
ATP + H2O + E217betaG/in
ADP + phosphate + E217betaG/out
show the reaction diagram
-
MRP3 preferentially transports E217betaG with a medium affinity and a very high capacity, while MRP1 transports E217betaG with a higher affinity but with much lower capacity
-
-
?
ATP + H2O + edaravone glucuronide/in
ADP + phosphate + edaravone glucuronide/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + epothilone B/in
ADP + phosphate + epothilone B/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + estradiol 17-beta-D-glucuronide/in
ADP + phosphate + estradiol 17-beta-D-glucuronide/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + estradiol glucuronide/in
ADP + phosphate + estradiol glucuronid/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + estrone-3-sulfate/in
ADP + phosphate + estrone-3-sulfate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + etoposide/in
ADP + phosphate + etoposide/out
show the reaction diagram
ATP + H2O + fexofenadine/in
ADP + phosphate + fexofenadine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + fluoxetine/in
ADP + phosphate + fluoxetine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + fluvoxamine/in
ADP + phosphate + fluvoxamine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + folic acid/in
ADP + phosphate + folic acid/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + furosemide/in
ADP + phosphate + furosemide/out
show the reaction diagram
ATP + H2O + gemcitabine/in
ADP + phosphate + gemcitabine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + glaucine/in
ADP + phosphate + glaucine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + glutathione/in
ADP + phosphate + glutathione/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + GSH-conjugated 4-hydroxy-nonenal/in
ADP + phosphate + GSH-conjugated 4-hydroxy-nonenal/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + GSH-conjugated prostaglandin/in
ADP + phosphate + GSH-conjugated prostaglandin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + Hoechst 33342/in
ADP + phosphate + Hoechst 33342/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + hydrochlorothiazide/in
ADP + phosphate + hydrochlorothiazide/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + hydroxyzine/in
ADP + phosphate + hydroxyzine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + indomethacin/in
ADP + phosphate + indomethacin/out
show the reaction diagram
ATP + H2O + leucovorin/in
ADP + phosphate + leucovorin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + leukotriene B4/in
ADP + phosphate + leukotriene B4/out
show the reaction diagram
-
MRP4 only transports leukotriene B4 in the presence of glutathione
-
-
?
ATP + H2O + leukotriene C4/in
ADP + phosphate + leukotriene C4/out
show the reaction diagram
ATP + H2O + leukotriene C4/in
ADP + phosphate + LTC4/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + leukotriene E4/in
ADP + phosphate + leukotriene E4/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + loperamide/in
ADP + phosphate + loperamide/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + loratadine/in
ADP + phosphate + loratadine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + lysophosphatidylinositol/in
ADP + phosphate + lysophosphatidylinositol/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + methotrexate/in
ADP + phosphate + methotrexate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + midazolam/in
ADP + phosphate + midazolam/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + misoprostol/in
ADP + phosphate + misoprostol/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + monensin/in
ADP + phosphate + monensin/out
show the reaction diagram
-
affinity of verapamil to MDR1 is not affected by pH value. Protein concentration is inversely related to the maximum activation of ATPase activity achieved
-
-
?
ATP + H2O + monoglucuronosyl bilirubin/in
ADP + phosphate + monoglucuronosyl bilirubin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + N-(1-phenylcyclohexyl)-3-ethoxypropanamine/in
ADP + phosphate + N-(1-phenylcyclohexyl)-3-ethoxypropanamine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + N-(2'-deoxy-beta-D-ribofuranosyl)-5-cyclohexyl-1H-indole/in
?
show the reaction diagram
-
nontransported substrate of P-glycoprotein
-
-
-
ATP + H2O + N-ethylmaleimide S-glutathione/in
ADP + phosphate + N-ethylmaleimide S-glutathione/out
show the reaction diagram
ATP + H2O + N-isopropyl-1,2-diphenylethylamine/in
ADP + phosphate + N-isopropyl-1,2-diphenylethylamine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + nicardipine/in
ADP + phosphate + nicardipine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + nifedipine/in
ADP + phosphate + nifedipine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + nortryptiline/in
ADP + phosphate + nortryptiline/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + olmesartan/in
ADP + phosphate + olmesartan/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + p-methoxy-ethylamphetamine/in
ADP + phosphate + p-methoxy-ethylamphetamine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + paclitaxel/in
ADP + phosphate + paclitaxel/out
show the reaction diagram
ATP + H2O + para-methoxy-ethylamphetamine/in
ADP + phosphate + para-methoxy-ethylamphetamine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + paroxetine/in
ADP + phosphate + paroxetine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + pirarubicin/in
ADP + phosphate + pirarubicin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + prazosin/in
ADP + phosphate + prazosin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + prednisone/in
ADP + phosphate + prednisone/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + probenecid/in
ADP + phosphate + probenecid/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + progesterone/in
ADP + phosphate + progesterone/out
show the reaction diagram
ATP + H2O + propoxyphene/in
ADP + phosphate + propoxyphene/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + prostaglandin A2/in
ADP + phosphate + prostaglandin A2/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + prostaglandin E1/in
ADP + phosphate + prostaglandin E1/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + prostaglandin E2/in
ADP + phosphate + prostaglandin E2/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + prostaglandin F2alpha/in
ADP + phosphate + prostaglandin F2alpha/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + puromycin/in
ADP + phosphate + puromycin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + quinidine/in
ADP + phosphate + quinidine/out
show the reaction diagram
ATP + H2O + repaglinide/in
ADP + phosphate + repaglinide/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + rhodamine 123 /in
ADP + phosphate + rhodamine 123 /out
show the reaction diagram
-
-
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
show the reaction diagram
ATP + H2O + rhodamine B/in
ADP + phosphate + rhodamine B/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + risperidone/in
ADP + phosphate + risperidone/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + ritonavir/in
ADP + phosphate + ritonavir/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + S-2,4-dinitrophenylglutathione/in
ADP + phosphate + S-2,4-dinitrophenylglutathione/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + salmeterol/in
ADP + phosphate + salmeterol/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + saquinavir/in
ADP + phosphate + saquinavir/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + sertraline/in
ADP + phosphate + sertraline/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + SN-38/in
ADP + phosphate + SN-38/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + sphingosine-1-phosphate/in
ADP + phosphate + sphingosine-1-phosphate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + talinolol/in
ADP + phosphate + talinolol/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + taurocholate/in
ADP + phosphate + taurocholate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + telmisartan/in
ADP + phosphate + telmisartan/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + tenofovir/in
ADP + phosphate + tenofovir/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + thromboxane B2/in
ADP + phosphate + thromboxane B2/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + topotecan/in
ADP + phosphate + topotecan/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + trazodone/in
ADP + phosphate + trazodone/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + urate/in
ADP + phosphate + urate/out
show the reaction diagram
ATP + H2O + ursodeoxycholylglycine/in
ADP + phosphate + ursodeoxycholylglycine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + ursodeoxycholyltaurine/in
ADP + phosphate + ursodeoxycholyltaurine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + valinomycin/in
ADP + phosphate + valinomycin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
show the reaction diagram
ATP + H2O + vinblastine sulfate/in
ADP + phosphate + vinblastine sulfate/out
show the reaction diagram
-
-
-
?
ATP + H2O + vinblastine/in
ADP + phosphate + vinblastine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + vincristine sulfate/in
ADP + phosphate + vincristine sulfate/out
show the reaction diagram
-
-
-
?
ATP + H2O + vincristine/in
ADP + phosphate + vincristine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + VP-16/in
ADP + phosphate + VP-16/out
show the reaction diagram
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
show the reaction diagram
ATP + H2O + zolpidem/in
ADP + phosphate + zolpidem/out
show the reaction diagram
-
-
-
-
?
colchicine/in + ATP + H2O
colchicine/out + ADP + phosphate
show the reaction diagram
-
-
-
?
cysteinyl leukotriene C4/in + ATP + H2O
cysteinyl leukotriene C4/out + ADP + phosphate
show the reaction diagram
-
-
-
?
daunorubicin/in + ATP + H2O
daunorubicin/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
dexamethasone/in + ATP + H2O
dexamethasone/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
digoxin/in + ATP + H2O
digoxin/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
doxorubicin/in + ATP + H2O
doxorubicin/out + ADP + phosphate
show the reaction diagram
estradiol 17-beta-D-glucuronide/in + ATP + H2O
estradiol 17-beta-D-glucuronide/out + ADP + phosphate
show the reaction diagram
etoposide/in + ATP + H2O
etoposide/out + ADP + phosphate
show the reaction diagram
-
-
-
?
glycocholate/in + ATP + H2O
glycocholate/out + ADP + phosphate
show the reaction diagram
-
-
-
?
leukotriene C4/in + ATP + H2O
leukotriene C4/out + ADP + phosphate
show the reaction diagram
leukotriene D4/in + ATP + H2O
leukotriene D4/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
leukotriene E4/in + ATP + H2O
leukotriene E4/out + ADP + phosphate
show the reaction diagram
-
-
-
?
methotrexate/in + ATP + H2O
methotrexate/out + ADP + phosphate
show the reaction diagram
-
-
-
?
N-(4',4'-azo-n-pentyl)-21-deoxy-ajamalinium/in + ATP + H2O
N-(4',4'-azo-n-pentyl)-21-deoxy-ajamalinium/out + ADP + phosphate
show the reaction diagram
-
-
-
?
nicardipine/in + ATP + H2O
nicardipine/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
paclitaxel/in + ATP + H2O
paclitaxel/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
rhodamine 123/in + ATP + H2O
rhodamine 123/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
rhodamine B/in + ATP + H2O
rhodamine B/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
S-(2,4-dinitrophenyl)glutathione/in + ATP + H2O
S-(2,4-dinitrophenyl)glutathione/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
valinomycin/in + ATP + H2O
valinomycin/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
verapamil/in + ATP + H2O
verapamil/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
vinblastine/in + ATP + H2O
vinblastine/out + ADP + phosphate
show the reaction diagram
-
-
-
-
?
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + H2O + 17beta-estradiol 17-(beta-D-glucuronide)/in
ADP + phosphate + 17beta-estradiol 17-(beta-D-glucuronide)/out
show the reaction diagram
ATP + H2O + 4-(2-aminoethyl)benzenesulfonylfluoride/in
ADP + phosphate + 4-(2-aminoethyl)benzenesulfonylfluoride/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 4-aminohippuric acid/in
ADP + phosphate + 4-aminohippuric acid/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + 5-(glutathione-S-yl)-N-methyl-alpha-methyldopamine/in
ADP + phosphate + 5-(glutathione-S-yl)-N-methyl-alpha-methyldopamine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + adefovir/in
ADP + phosphate + adefovir/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + allopurinol/in
ADP + phosphate + allopurinol/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + calcein/in
ADP + phosphate + calcein/out
show the reaction diagram
-
fluorescent substrate of MRP1
-
-
?
ATP + H2O + cAMP/in
ADP + phosphate + cAMP/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cefazolin/in
ADP + phosphate + cefazolin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cefmetazole/in
ADP + phosphate + cefmetazole/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cefotaxime/in
ADP + phosphate + cefotaxime/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + ceftizoxime/in
ADP + phosphate + ceftizoxime/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + celecoxib/in
ADP + phosphate + celecoxib/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cGMP/in
ADP + phosphate + cGMP/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + chenodeoxycholylglycine/in
ADP + phosphate + chenodeoxycholylglycine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + chenodeoxycholyltaurine/in
ADP + phosphate + chenodeoxycholyltaurine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cholate/in
ADP + phosphate + cholate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cholesterol/in
ADP + phosphate + cholesterol/out
show the reaction diagram
-
P-gp may actively mediate cholesterol redistribution in the cell membrane, P-gp mediates the ATP-dependent relocation of cholesterol from the cytosolic leaflet to the exoplasmic leaflet of the plasma membrane, P-gp likely contributes in stabilizing the cholesterol-rich microdomains, rafts and caveolae, and is involved in the regulation of cholesterol trafficking in cells
-
-
?
ATP + H2O + cholylglycine/in
ADP + phosphate + cholylglycine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + cholytaurine/in
ADP + phosphate + cholytaurine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + daunorubicin/in
ADP + phosphate + daunorubicin/out
show the reaction diagram
-
fluorescent substrate of P-glycoprotein
-
-
?
ATP + H2O + dehydroepiandrosterone sulfate/in
ADP + phosphate + dehydroepiandrosterone sulfate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + deoxycholylglycine/in
ADP + phosphate + deoxycholylglycine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + dipyridamole/in
ADP + phosphate + dipyridamole/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + doxorubicin/in
ADP + phosphate + doxorubicin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + edaravone glucuronide/in
ADP + phosphate + edaravone glucuronide/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + estrone-3-sulfate/in
ADP + phosphate + estrone-3-sulfate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + furosemide/in
ADP + phosphate + furosemide/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + GSH-conjugated 4-hydroxy-nonenal/in
ADP + phosphate + GSH-conjugated 4-hydroxy-nonenal/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + GSH-conjugated prostaglandin/in
ADP + phosphate + GSH-conjugated prostaglandin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + hydrochlorothiazide/in
ADP + phosphate + hydrochlorothiazide/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + indomethacin/in
ADP + phosphate + indomethacin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + leucovorin/in
ADP + phosphate + leucovorin/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + leukotriene B4/in
ADP + phosphate + leukotriene B4/out
show the reaction diagram
-
MRP4 only transports leukotriene B4 in the presence of glutathione
-
-
?
ATP + H2O + leukotriene C4/in
ADP + phosphate + leukotriene C4/out
show the reaction diagram
ATP + H2O + leukotriene C4/in
ADP + phosphate + LTC4/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + leukotriene E4/in
ADP + phosphate + leukotriene E4/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + lysophosphatidylinositol/in
ADP + phosphate + lysophosphatidylinositol/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + methotrexate/in
ADP + phosphate + methotrexate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + olmesartan/in
ADP + phosphate + olmesartan/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + p-methoxy-ethylamphetamine/in
ADP + phosphate + p-methoxy-ethylamphetamine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + paclitaxel/in
ADP + phosphate + paclitaxel/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + probenecid/in
ADP + phosphate + probenecid/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + prostaglandin A2/in
ADP + phosphate + prostaglandin A2/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + prostaglandin E1/in
ADP + phosphate + prostaglandin E1/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + prostaglandin E2/in
ADP + phosphate + prostaglandin E2/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + prostaglandin F2alpha/in
ADP + phosphate + prostaglandin F2alpha/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
show the reaction diagram
ATP + H2O + sphingosine-1-phosphate/in
ADP + phosphate + sphingosine-1-phosphate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + taurocholate/in
ADP + phosphate + taurocholate/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + tenofovir/in
ADP + phosphate + tenofovir/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + thromboxane B2/in
ADP + phosphate + thromboxane B2/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + topotecan/in
ADP + phosphate + topotecan/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + urate/in
ADP + phosphate + urate/out
show the reaction diagram
-
MRP4 is the first secretory transporter identified in the bidirectional renal handling of urate and could be a potential drug target in the treatment of hyperuricaemia, regulation, overview
-
-
?
ATP + H2O + ursodeoxycholylglycine/in
ADP + phosphate + ursodeoxycholylglycine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + ursodeoxycholyltaurine/in
ADP + phosphate + ursodeoxycholyltaurine/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
show the reaction diagram
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
show the reaction diagram
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(17beta)-N-([trans-4-[(6-amino-9H-purin-9-yl)methyl]cyclohexyl]methyl)-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 99% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[(2E)-4-(6-amino-9H-purin-9-yl)but-2-en-1-yl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 72% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[(2Z)-4-(6-amino-9H-purin-9-yl)but-2-en-1-yl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 86% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[4-(6-amino-9H-purin-9-yl)but-2-yn-1-yl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 61% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[4-(6-amino-9H-purin-9-yl)butyl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 78% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[4-[(6-amino-9H-purin-9-yl)methyl]benzyl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 98% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[6-(6-amino-9H-purin-9-yl)hexyl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 111% of the accumulation in presence of 0.01 mM progesterone
(1beta,1'beta)-5-bromo-6,6',7,12-tetramethoxy-2-methylberbaman
-
is an effectively and potential agent in reversing Pgp-mediated multidrug resistance by inhibiting the transport function and expression of Pgp
(2aR,6aR,12bS,14bS)-10,17-dimethoxy-3,3,6,6-tetramethyl-2a,3,6a,7,12b,14b-hexahydro-2H,6H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[3,2-h]chromene-13,14-dione
-
inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells
(2aR,6aS,12bR,14bS)-10,17-dimethoxy-3,3,6,6-tetramethyl-2a,3,6a,7,12b,14b-hexahydro-2H,6H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[3,2-h]chromene-13,14-dione
-
inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells
(2R,4aR,7bR,9R,11aR,14bR)-2,5,5,9,12,12-hexamethyl-1,3,4,4a,5,8,9,10,11,11a,12,14b-dodecahydrobenzo[c]isochromeno[3,4-g]chromene-7,14(2H,7bH)-dione
-
inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells
(6aS,9bR,15aS,18bR)-2,4,11,13-tetrabromo-7,7,16,16-tetramethyl-6a,15a,16,18b-tetrahydro-6H,15H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[2,3-g]chromene-9,18(7H,9bH)-dione
-
inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells
(6aS,9bR,15aS,18bR)-3,12-dimethoxy-7,7,16,16-tetramethyl-6a,15a,16,18b-tetrahydro-6H,15H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[2,3-g]chromene-9,18(7H,9bH)-dione
-
inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells
(R)-4-[(1a,6,10b)-1,1-dichloro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-[(5-quinolinyloxy)methyl]-1-piperazineethanol
-
complete inhibition of P-glycoprotein at 0.005 mM
-
(R)-4-[(1a,6,10b)-1,1-difluoro-1,1a,6,10btetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-[(5-quin-olinyloxy)methyl]-1-piperazineethanol
-
LSN 335979, P-glycoprotein-specific inhibitor
-
1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane
-
competitive inhibitor to doxorubicin binding by P-glycoprotein
-
1-(4-acetylpiperazin-1-yl)-4-propoxy-9H-thioxanthen-9-one
-
uncompetitive, approximately 1.5fold more potent than verapamil in decreasing the doxorubicin GI50 on K-562 Dox cell line
1-isatin-4-(40-methoxyphenyl)-3-thiosemicarbazone
-
IC50 against KB-3-1 cells 0.0142 mM, against KB-VI cells 0.0033 mM. Displays MDR1-selectivity against all P-glycoprotein expressing cell lines examined, and cross-resistance is no observed. Selectivity is reversed by inhibitors of P-glycoprotein ATPase activity. Compound also shows selectivity for cells expressing mouse and hamster MDR1
1-isatin-4-(40-nitrophenyl)-3-thiosemicarbazone
-
IC50 against KB-3-1 cells 0.0171 mM, against KB-VI cells 0.0021 mM
1-isatin-4-(40-tert-butyl phenyl)-3-thiosemicarbazone
-
IC50 against KB-3-1 cells 0.0159 mM, against KB-VI cells 0.0148 mM
1-[[2-(4-nitrophenyl)ethyl]amino]-4-propoxy-9H-thioxanthen-9-one
-
uncompetitive, approximately 1.5fold more potent than verapamil in decreasing the doxorubicin GI50 on K-562 Dox cell line
10-(3-(dimethylamino)propyl)-2-(trifluoromethyl)phenothiazine
-
-
16alpha-17beta-estradiol 17-(beta-D-glucuronide)
-
transport of aflatoxin B1-epoxide-GSH conjugate
17-beta-estradiol 17-beta-(D-glucuronide)
17beta-estradiol 16-(beta-D-glucuronide)
-
transport of aflatoxin B1-epoxide-GSH conjugate
17beta-estradiol 3-sulfato-17-(beta-D-glucuronide)
-
transport of aflatoxin B1-epoxide-GSH conjugate
2,6-bis(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonothioyl)thien-2-yl)thiopyrylium chloride
-
81% inhibition of MRP1 at 0.01 mM
-
2,6-bis(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonyl)thien-2-yl)thiopyrylium hexafluorophosphate
-
78% inhibition of MRP1 at 0.01 mM
-
2,6-di-tert-butyl-4-(5-(piperidine-1-carbonothioyl)thien-2-yl)thiopyrylium hexafluorophosphate
-
11% inhibition of MRP1 at 0.01 mM
-
2,6-di-tert-butyl-4-(5-(piperidine-1-carbonothioyl)thiophen-2-yl)thiopyrylium chloride
-
32% inhibition of MRP1 at 0.01 mM
-
2-(4-maleimidoanilino)-naphthalene-6-sulfonic acid
-
-
-
2-tert-butyl-6-(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonothioyl)thiophen-2-yl)thiopyrylium chloride
-
93% inhibition of MRP1 at 0.01 mM
-
2-tert-butyl-6-(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonyl)thien-2-yl)thiopyrylium hexafluorophosphate
-
59% inhibition of MRP1 at 0.01 mM
-
2-[4-(3-ethoxy-1-propenyl)phenyl]-4,5-bis-[4-(2-propylamino)phenyl]-1H-imidazole
-
i.e. OC144-093. Coadministration of OC144-093 with docetaxel enhances the oral bioavailability of docetaxel to a limited extent (8-26%) in humans, and has a good safety profile as well
3-[(3-[[(1,3-dioxo-8-phenyl-3,3a,3b,8,8a,8b-hexahydroindeno[1',2':3,4]cyclobuta[1,2-c]pyrrol-2(1H)-yl)acetyl]oxy]propyl)(methyl)amino]propyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
3-[(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl (2E)-3-(anthracen-9-yl)prop-2-enoate
-
-
3-[(3-[[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]oxy]propyl)(methyl)amino]propyl 10-chloroanthracene-9-carboxylate
-
-
3-[(3-[[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]oxy]propyl)(methyl)amino]propyl 3,4,5-trimethoxybenzoate
-
-
3-[(3-[[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]oxy]propyl)(methyl)amino]propyl anthracene-9-carboxylate
-
-
3-[(3-[[3-(1,3-dioxo-8-phenyl-3,3a,3b,8,8a,8b-hexahydroindeno[1',2':3,4]cyclobuta[1,2-c]pyrrol-2(1H)-yl)propanoyl]oxy]propyl)(methyl)amino]propyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
3-[(3-[[3-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)propanoyl]oxy]propyl)(methyl)amino]propyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
3-[(3-[[bis(4-methoxyphenyl)acetyl]oxy]propyl)(methyl)amino]propyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl (2E)-3-(3,4-dimethoxyphenyl)prop-2-enoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl (2E)-3-(anthracen-9-yl)prop-2-enoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl (2E)-3-(biphenyl-4-yl)prop-2-enoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl 3,3-diphenylprop-2-enoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl 3,4,5-trimethoxybenzoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl anthracene-9-carboxylate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl biphenyl-4-carboxylate
-
-
3-[[3-[(diphenylacetyl)oxy]propyl](methyl)amino]propyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
4-(2-aminoethyl)benzenesulfonylfluoride
-
-
4-[5-(4-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide
-
i.e. SC236. The direct inhibitory effects of indomethacin and SC236 on P-gp may contribute to their ability to increase the intracellular retention of doxorubicin and thus enhance its cytotoxicity
5'-O-[4-(fluorosulfonyl)benzoyl]adenosine
-
incubation inhibits ATP hydrolysis and the binding of 8-azido-ATP. 5'-Fluorosulfonylbenzoyl 5'-adenosine is an ATP analog that interacts with both the drug-binding and ATP-binding sites of P-gp, but fluorosulfonyl-mediated crosslinking is observed only at the nucleotide-binding domains
5-[(5-[[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]oxy]pentyl)(methyl)amino]pentyl 3,4,5-trimethoxybenzoate
-
-
5-[(5-[[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]oxy]pentyl)(methyl)amino]pentyl anthracene-9-carboxylate
-
-
5-[(5-[[bis(4-methoxyphenyl)acetyl]oxy]pentyl)(methyl)amino]pentyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
5-[methyl(5-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]pentyl)amino]pentyl (2E)-3-(biphenyl-4-yl)prop-2-enoate
-
-
5-[methyl(5-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]pentyl)amino]pentyl 3,3-diphenylprop-2-enoate
-
-
8-prenylnaringenin
-
-
9,10-dihydro-5-methoxy-9-oxo-N-{4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]phenyl}-4-acridine
-
i.e. GF120918. A good and safe P-gp inhibitor alternative for cyclosporin A in enhancing the oral bioavailability of paclitaxel
abamectin
-
-
acacetin
-
-
acitretin
-
-
apigenin
-
-
arsenate
-
competitive inhibitor of daunorubicin transport
auraptene
-
stimulates the ATPase activity of MRP1. No inhibition of MRP1-mediated efflux by auraptene, but auraptene increases the accumulation of daunorubicin in KB-C2 cells
azido-ATP
-
competitive, binding activity of wild-type and mutant enzymes, overview
azidophenacylglutathione
-
competitive inhibitor of daunorubicin transport
benzbromarone
beta-sitosterol-O-glucoside
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
bisoprolol
-
-
bis[(4aS,6R,8aS)-3-methoxy-11-methyl-5,6,9,10,11,12-hexahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-6-yl] decanedioate
-
galactamine dimer. the inhibitory activity of the inhibitor on P-gp transport of substrate is evaluated in cells that over-express P-gp
buprenorphine
-
inhibits paclitaxel transport, placental brush border membrane vesicles
byakangelicol
-
shows strong P-gp inhibition from the screening of P-gp inhibitor evaluated by quinidine permeation through the Caco-2 monolayer
carnosic acid
-
increases the accumulation of daunorubicin or rhodamine 123 in KB-C2 cells. The ATPase activity of P-glycoprotein is stimulated
carnosol
-
increases the accumulation of daunorubicin or rhodamine 123 in KB-C2 cells. The ATPase activity of P-glycoprotein is stimulated
carvedilol
-
-
celecoxib
-
-
cholecalciferol
-
-
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
cis-(Z)-flupentixol
-
is a non-competitive inhibitor that interacts with the substrate site but is not transported
curcumin
-
modulates Pgp expression
cyclosporin A
cyclosporine A
-
-
D-alpha-tocopheryl polyethylene glycol 1000 succinate
-
i.e. TPGS 1000, water-soluble Vitamin E derivative. Inhibits substrate-induced ATPase activity without inducing significant ATPase activity on its own. Modulation of ATPase activity correlates with inhibitory potential for P-glycoprotein-mediated efflux
-
deacetylnomilin
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
desloratadine
-
weakly inhibits daunorubicin transport, 19% of the inhibition caused by vanadate, IC50: 0.043 nM, desloratadine is no significant inhibitor of P-gp and should not cause clinical drug interactions with agents that are P-gp substrates
diclofenac
-
inhibits MRP2-mediated drug transport
Digitonin
-
inhibits ATPase activity of P-gp
dipyridamole
-
; potent inhibition of MRP4
doxorubicin
-
cis-inhibition without trans-inhibition on MDR1-mediated vinblastine efflux of Xenopus laevis oocytes expressing human P-glycoprotein
EDTA
-
-
elacridar
-
GF120918
flavonoids
-
useful inhibitors for clinical application to multidrug resistance
flurazepam
-
inhibits daunorubicin efflux up to 80%, partially inhibits ATPase activity
genistein
-
competitive inhibitor of daunorubicin transport
glibenclamide
-
mutation of residue Tyr2 in MRP1 cannot alter the sensitivity to glibenclamide
gomisin A
-
strongly inhibits P-glycoprotein ATPase activity in cells overexpressing the enzyme. Alters substrate interaction of P-glycoprotein but itself is neither a substrate nor a competitive inhibitor
HEPES
-
uptake of P-glycoprotein substrates is substantially diminished when the HEPES concentration is raised to 25 mM. Addition of 15 or 25 mM HEPES in the uptake buffer results in significant reduction in the accumulation of P-glycoprotein substrates cyclosporine-A, ritonavir, and lopinavir. Bidirectional A-B and B-A transport studies show that permeability ratio in the presence of 25 mM HEPES is significantly higher than control. HEPES stimulates the production of ATP and modulates the energy dependent efflux and uptake processes
hesperidin
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
indomethacin
Ko143
-
-
-
KR30031
-
-
laniquidar
-
R101933
leukotriene D4
-
transport of aflatoxin B1-epoxide-GSH conjugate
limonin
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
loratadine
-
inhibits daunorubicin transport, IC50: 0.011 nM, much less inhibitory than cyclosporin A or verapamil, 43% of the inhibition caused by vanadate
losartan
-
-
lovastatin
-
increases the absorption of verapamil (used as an antiarrhythmic agent to control supraventricular tachyarrhythmias) by inhibiting P-glycoprotein
methadone
-
inhibits paclitaxel transport, placental brush border membrane vesicles
methoxypolyethylene17 glycol-beta-caprolactone5
-
amphiphilic diblock copolymer, decreases membrane fluidity and inhibits enzyme-mediated efflux while stimulating the enzyme's ATPase activity up to 3fold
methyl-beta-cyclodextrin
-
inhibits ATPase activity of P-gp, 5-10 mM, total inhibition
miconazole
-
-
misoprostol
-
-
MK-571
MK571
monoclonal antibiodies
-
morin
-
-
myricetin
-
-
N-(2'-deoxy-beta-D-ribofuranosyl)-5-cyclohexyl-1H-indole
-
nontransported substrate of P-glycoprotein
N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate
-
-
N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-selenoxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate
-
-
N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-telluroxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate
-
-
N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-thioxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate
-
-
N-[9-[3-(dimethylamino)phenyl]-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene]-N-methylmethanaminium bromide
-
-
N-[9-[4-(dimethylamino)phenyl]-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene]-N-methylmethanaminium bromide
-
-
nafcillin
-
-
nanoparticles
-
doxorubicin and paclitaxel nanoparticles inhibit P-glycoprotein and transiently deplete ATP, while cyclosporine A and polystyrene nanoparticles do not, overview
-
naringin
-
i.e. 7-[[2-O-(6-deoxy-alpha-L-mannopyra nosyl)-beta-D-glucopyranosyl]oxy]-2,3-dihydro-5-hydroxy-2-(4-hydroxyphenyl)-4H-1-benzo pyran-4-one. Pre-treatment with naringin prior to doxorubicin treatment increases the sensitivity of the enzyme to doxorubicin, naringin inhibits the doxorubicin-stimulated ATPase activity and may interact directly with the transporter. Naringin seems to modulate the in vivo expression of P-gp
neohesperidin
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
nigericin
-
-
nobiletin
-
a chemopreventive citrus phytochemical from orange, stimulates the ATPase activity of MRP1. Nobiletin also increases the accumulation of calcein, a fluorescent substrate of MRP1, in KB/MRP cells, and of P-glycoprotein substrate daunorubicin in KB-C2 cells
ortho-vanadate
-
specific inhibitor
orthovanadate
-
non-covalent inhibitor of ABC ATPases catalyzing a photo-oxidative cleavage, characterization of three cleavage sites within MRP1, influence of nucleotides and transported substrates on the cleavage reaction, mechanism
praeruptorin A
-
modulates Pgp expression
probenecid
-
-
progesterone
Promethazine
-
-
propranolol
-
-
PSC833
quercetin
-
-
quinidine
-
trans-inhibition on MDR1-mediated vinblastine and digoxin efflux of Xenopus laevis oocytes expressing human P-glycoprotein
repaglinide
-
-
rivulobirin A
-
shows strong P-gp inhibition from the screening of P-gp inhibitor evaluated by quinidine permeation through the Caco-2 monolayer
S-butyl glutathione
-
transport of aflatoxin B1-epoxide-GSH conjugate
S-decyl-glutathione
S-hexyl glutathione
-
transport of aflatoxin B1-epoxide-GSH conjugate
S-octyl glutathione
-
transport of aflatoxin B1-epoxide-GSH conjugate
salinomycin
-
treatment of the multidrug resistant cell lines with salinomycin restores a normal drug sensitivity of these cells
salmeterol
-
-
semi-beta-carotene-epoxide
-
-
sildenafil
-
; potent inhibition of MRP4
stigmasterol
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
sulfinpyrazone
-
-
sulindac
-
-
tariquidar
-
XR9576
telmisartan
-
-
tert-butyl (4R)-4-(benzyloxy)-1-(tert-butoxycarbonyl)-L-prolyl-N6-[(benzyloxy)carbonyl]-L-lysinate
-
noncompetitive inhibitor towards daunorubicin and Hoechst 33342
tetrahydrocurcumin
-
inhibitory to P-glycoprotein as well as to mitoxantrone resistance protein and multidrug resistance protein1. Inhibition of transport function with concomitant stimulation of ATPase activity
tetrandrine
tomato lectin
-
-
-
trans,trans-4,17(20)-pregnadiene-3,16-dione
-
i.e. Z-guggulsterone. In presence of guggulsterone, fluorescent substrates daunorubicin or rhodamine 123 accumulate in KB-C2 cells. Efflux of rhodamine 123 is inhibited and the accumulation of substrate calcein is increased. ATPase activities of both isoforms ABCB1 And ABCC1 are stimulated
ursolic acid
-
increases the accumulation of daunorubicin or rhodamine 123 in KB-C2 cells. The ATPase activity of P-glycoprotein is stimulated
valspodar
-
-
-
vanadate
verapamil
vinblastine
-
-
vincristine
-
alone is a very poor inhibitor of transport of leukotriene C4, together with GSH acts as relatively potent competitive inhibitor
wogonin
-
impairs the function of P-glycoprotein and increases cellular content of etoposide in HL-60 cells. Wogonin may be used to reduce the excretion of anticancer agents via P-glycoprotein and to increase the pharmacological action in cancer cells. Wogonin may play a role in overcoming multidrug resistance
XR9576
-
is a non-competitive inhibitor that interacts with the substrate site but is not transported
zosuquidar
[2-(1H-benzimidazol-2-yl)ethanamine]-4-propoxy-9H-thioxanthen-9-one
-
uncompetitive, causes an accumulation rate of rhodamine-123 similar to that caused by verapamil in the K-562 Dox resistant cell line, and a decrease in ATP consumption by P-gp. At 10 mM, 12.5fold decrease in the GI50 value of doxorubicin in the K-562 Dox resistant cell line, being 2fold more potent than verapamil
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane
-
stimulates ATPase activity by 2.7-fold
-
2,5-dimethoxy-4-iodoamphetamine
-
-
-
2-methyl-GSH
-
supports transport of vincristine
-
3,4-methylenedioxy-alpha-ethylphenethylamine
-
-
-
3-doxyl-17beta-hydroxy-5alpha-androstane
-
stimulation of ATPase-activity arising from co-expression of isoforms ABCG5 and ABCG8
4-androstene-3,17-dione
-
stimulation of ATPase-activity arising from co-expression of isoforms ABCG5 and ABCG8
5-androsten-3beta-ol-17-one
-
stimulation of ATPase-activity arising from co-expression of isoforms ABCG5 and ABCG8
auraptene
-
stimulates the ATPase activity of MRP1. No inhibition of MRP1-mediated efflux by auraptene, but auraptene increases the accumulation of daunorubicin in KB-C2 cells
benzbromarone
Berberine
-
about 4fold stimulation of ATPase activity
bromazepam
-
stimulation of ATPase activity, no effect on daunorubicin efflux
campesterol
-
enhances paclitaxel-stimulated ATPase activity of enzyme
Chlordiazepoxide
-
stimulation of ATPase activity, no effect on daunorubicin efflux
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
Colchicine
-
450 microM, 50% stimulation
diazepam
-
stimulation of ATPase activity, no effect on daunorubicin efflux
diclofenac
-
MRP2-mediated transport of amphipathic lipophilic drugs, stimulates paclitaxel, docetaxel, and saquinavir transport
doxorubicin
-
activates and induces the enzyme
ginsenoside Rh1
-
-
glaucine
-
-
-
glutathione
hydrastine
-
about 2.5fold stimulation of ATPase activity
methoxypolyethylene17 glycol-beta-caprolactone5
-
amphiphilic diblock copolymer, decreases membrane fluidity and inhibits enzyme-mediated efflux while stimulating the enzyme's ATPase activity up to 3fold
MK571
-
slightly activates E217betaG activated ATPase activity of MRP3 at 0.01-0.05 mM and N-ethylmaleimide S-glutathione activated ATPase activity of MRP1 at 500-2000 nM, but inhibits MRP1 activity half-maximally at 0.01 mM, MK571 may be a potential transported substrate for MRP3, 20% stimulation of E217betaG uptake by MRP1 at 500-1000 nM, but inhibits this activity at 0.01-0.05 mM, stimulates E217betaG uptake by MRP3 at 0.002-0.005 mM, but inhibits this activity at 0.05-0.1 mM
monensin
-
protein concentration of enzyme is inversely related to the maximum activation of ATPase activity achieved
N-(1-phenylcyclohexyl)-3-ethoxypropanamine
-
-
-
N-isopropyl-1,2-diphenylethylamine
-
-
-
nicardipine
-
-
nobiletin
-
a chemopreventive citrus phytochemical from orange, stimulates the ATPase activity of MRP1. Nobiletin also increases the accumulation of calcein, a fluorescent substrate of MRP1, in KB/MRP cells
quinidine
-
protein concentration of enzyme is inversely related to the maximum activation of ATPase activity achieved
rhodamine B
-
44 microM, 50% stimulation
rhodamine derivatives
-
enhancement of calcein uptake into MDCK-MDR1 cells by diverse rhodamine analogues, detailed overview
-
rosamine derivatives
-
enhancement of calcein uptake into MDCK-MDR1 cells by diverse rosamine analogues, detailed overview
-
S-butyl-GSH
-
supports transport of vincristine
S-ethyl-GSH
-
supports transport of vincristine
schisandrol A
-
isolated from fruit of Schisandra chinensis. Increases cellular retention of P-glycoprotein substrates such as rhodamine 123. Schisandrol A stimulates basal P-glycoprotein ATPase activity, is not competitive to verapamil or progesterone and decreases their Km value without changing Vmax values
sertraline
-
-
sitosterol
-
enhances paclitaxel-stimulated ATPase activity of enzyme
stigmasterol
-
enhances paclitaxel-stimulated ATPase activity of enzyme
tetrahydrocurcumin
-
inhibitory to P-glycoprotein as well as to mitoxantrone resistance protein and multidrug resistance protein1. Inhibition of transport function with concomitant up to 2.6fold stimulation of ATPase activity
trans,trans-4,17(20)-pregnadiene-3,16-dione
-
i.e. z-guggulsterone, stimulation of ATPase activity, inhibitory to substrate transport
verapamil
vinblastine
vincristine
-
stimulates transport of GSH
additional information
-
elevated levels of hepatic MRP4 are found after hepatotoxicant exposure, probably mediated via transcription factor NFE2-related factor 2. Human cells upregulate MRP4 after long-term exposure to nucleoside-based drugs
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.195
17beta-estradiol 17-(beta-D-glucuronide)
-
pH 7.0, 37C, recombinant MRP2
0.016 - 0.0242
17beta-glucuronosyl [6,7-3H]oestradiol
0.0057
2,4-dinitrophenyl S-glutathione/in
-
-
0.108
2,4-dinitrophenyl-S-glutathione
-
pH 7.0, 37C, recombinant MRP2
0.0027
2,5-dimethoxy-4-iodoamphetamine/in
-
at pH 6.8 and 37C
-
0.0046
3,4-methylenedioxy-alpha-ethylphenethylamine/in
-
at pH 6.8 and 37C
-
0.000189
aflatoxin B1-epoxide-GSH conjugate/in
-
-
0.0009 - 2.37
ATP
0.0031
calcein/in
-
37C, pH not specified in the publication
0.037 - 0.72
colchicine/in
0.36 - 2
cyclic guanosine monophosphate/in
0.0004
cyclosporine A/in
-
37C, pH not specified in the publication
0.0061
daunorubicin/in
-
-
0.394 - 0.826
dexamethasone
0.076 - 0.181
digoxin
0.101 - 0.187
digoxin/in
0.00085
doxorubicin/in
-
37C, pH not specified in the publication
0.008 - 0.035
E217betaG
0.013 - 0.17
estradiol 17-beta-D-glucuronide/in
0.134
Estrone 3-sulfate
-
pH 7.0, 37C, recombinant MRP2
0.0057
etoposide/in
-
-
0.13 - 0.26
folic acid/in
0.0071
glaucine/in
-
at pH 6.8 and 37C
-
0.248
glycocholate/in
-
-
0.0109
leukotriene C4
-
pH 7.0, 37C, recombinant MRP2
0.000036 - 0.0053
leukotriene C4/in
4.522
methotrexate
-
pH 7.0, 37C, recombinant MRP2
0.24 - 0.776
methotrexate/in
0.0037
N-(1-phenylcyclohexyl)-3-ethoxypropanamine/in
-
at pH 6.8 and 37C
-
0.00006
N-(2'-deoxy-beta-D-ribofuranosyl)-5-cyclohexyl-1H-indole/in
-
37C, pH not specified in the publication
0.3
N-ethylmaleimide S-glutathione
-
pH 7, 37C, MRP1
0.0046
N-isopropyl-1,2-diphenylethylamine/in
-
at pH 6.8 and 37C
-
0.001 - 0.0026
nicardipine
0.000383 - 0.00191
nicardipine/in
0.0013 - 0.0016
paclitaxel
0.000665 - 0.0009
paclitaxel/in
0.351
probenecid
-
pH 7.0, 37C, recombinant MRP2
0.00377 - 0.0207
progesterone/in
0.00788
quinidine
-
pH 6.8, 37C
0.01 - 0.021
rhodamine 123
0.0118 - 0.0354
rhodamine 123/in
0.007 - 0.014
rhodamine B
0.0109 - 0.0298
rhodamine B/in
0.006
sertraline/in
-
at pH 6.8 and 37C
0.0022 - 0.0035
valinomycin
0.0022 - 0.0115
verapamil
0.000614 - 0.00579
verapamil/in
0.0013 - 0.052
vinblastine
0.0002 - 0.1455
vinblastine/in
0.0027 - 0.0039
vincristine
0.0055
vincristine/in
-
-
0.0346 - 0.0463
[1,2,6,7-3H(N)]dehydroepiandrosterone-3-sulfate
additional information
additional information
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.189 - 2.95
ATP
1.25 - 7.81
colchicine/in
0.791 - 5.99
digoxin/in
3.48 - 8.44
nicardipine/in
1.3 - 2.2
paclitaxel/in
1.84 - 8.56
rhodamine 123/in
2.23 - 7.22
rhodamine B/in
5.8
verapamil
Homo sapiens
-
pH 7.4, 37C, EPR spin-labeled verapamil
3.28 - 8.27
verapamil/in
1.9 - 6.54
vinblastine/in
additional information
additional information
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1.66 - 28.2
colchicine/in
8394
4.23 - 59.2
digoxin/in
9930