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Information on EC 7.6.2.3 - ABC-type glutathione-S-conjugate transporter and Organism(s) Homo sapiens and UniProt Accession O15440

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IUBMB Comments
A eukaryotic ATP-binding cassette (ABC) type transporter that mediates the transport of glutathione-S-conjugates. The mammalian enzyme, which also transports some glucuronides, exports the substrates out of the cell, while plant and fungal transporters export them into the vacuole. Over-expression confers resistance to anticancer drugs by their efficient exportation in glutathione-S-conjugate form.
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This record set is specific for:
Homo sapiens
UNIPROT: O15440
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
organic anion transporting polypeptide, rlip76, mrp-1, oatp2, oatp1, abcc5, gsh transporter, hgt1p, multidrug resistance associated protein 2, mrp transporter, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glutathione S-conjugate transporter
-
GSH transporter
-
multidrug resistance-associated protein
-
ABCC1
ABCC2
ABCC3
ABCC4
Abcc5
Q15440
-
breast cancer resistance protein
canalicular MRP
-
canalicular multispecific organic anion transporter
-
glutathione S-conjugate transporter
-
glutathione-conjugate transporter
-
-
glutathione-S-conjugate-translocating ATPase
-
-
-
-
GSH transporter
-
Mpr7
-
-
Mpr8
-
-
MRP
-
-
-
-
MRP transporter
-
-
MRP5
Q15440
-
MRP6
isoform
multidrug resistance associated protein 2
-
multidrug resistance associated protein-1
-
multidrug resistance protein
-
multidrug resistance protein 1
multidrug resistance protein 2
-
multidrug resistance protein transporter
-
-
multidrug resistance-associated protein
multidrug resistance-associated protein 1
multidrug resistance-associated protein 2
-
multidrug-resistance protein 1
-
P-glycoprotein
-
P-glycoprotein-1
-
YBT1
-
-
-
-
Ycf1
-
-
-
-
PATHWAY SOURCE
PATHWAYS
-
-, -, -, -, -
SYSTEMATIC NAME
IUBMB Comments
ATP + H2O + glutathione-S-conjugate[side 1] = ADP + phosphate + glutathione-S-conjugate[side 2]
A eukaryotic ATP-binding cassette (ABC) type transporter that mediates the transport of glutathione-S-conjugates. The mammalian enzyme, which also transports some glucuronides, exports the substrates out of the cell, while plant and fungal transporters export them into the vacuole. Over-expression confers resistance to anticancer drugs by their efficient exportation in glutathione-S-conjugate form.
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 + glutathione-S-conjugate[side 1]
ADP + phosphate + glutathione-S-conjugate[side 2]
show the reaction diagram
ATP + H2O + leukotriene C4[side 1]
ADP + phosphate + leukotriene C4[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(6-mercaptopurinyl)glutathione[side 1]
ADP + phosphate + S-(6-mercaptopurinyl)glutathione[side 2]
show the reaction diagram
substrate for isoforms MRP4 and MRP5
-
-
?
ATP + H2O + S-(6-thioguaninyl)glutathione[side 1]
ADP + phosphate + S-(6-thioguaninyl)glutathione[side 2]
show the reaction diagram
substrate for isoforms MRP4 and MRP5
-
-
?
ATP + H2O + (+)-10R-(S-glutathionyl)-7S,8R,9R-trihydroxy-7,8,9,10-tetrahydrobenzo[a]pyrene[side 1]
ADP + phosphate + (+)-10R-(S-glutathionyl)-7S,8R,9R-trihydroxy-7,8,9,10-tetrahydrobenzo[a]pyrene[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + (-)-10S-(S-glutathionyl)-7R,8S,9S-trihydroxy-7,8,9,10-tetrahydrobenzo[a]pyrene[side 1]
ADP + phosphate + (-)-10S-(S-glutathionyl)-7R,8S,9S-trihydroxy-7,8,9,10-tetrahydrobenzo[a]pyrene[side 2]
show the reaction diagram
best substrate
-
-
?
ATP + H2O + (aryl-azido)-glutathione[side 1]
ADP + phosphate + (aryl-azido)-glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + (iodoaryl-azido)-glutathione[side 1]
ADP + phosphate + (iodoaryl-azido)-glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + 2,4-dinitrophenyl-S-glutathione[side 1]
ADP + phosphate + 2,4-dinitrophenyl-S-glutathione[side 2]
show the reaction diagram
ATP + H2O + 3'-(3-methoxymorpholino)doxorubicin[side 1]
ADP + phosphate + 3'-(3-methoxymorpholino)doxorubicin[side 2]
show the reaction diagram
about 106% activity
-
-
?
ATP + H2O + 4-(glutathione-S-yl)-quinoline-1-oxide[side 1]
ADP + phosphate + 4-(glutathione-S-yl)-quinoline-1-oxide[side 2]
show the reaction diagram
ATP + H2O + 4-hydroxynonenal-glutathione[side 1]
ADP + phosphate + 4-hydroxynonenal-glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + 5-(glutathion-S-yl)-N-methyl-alpha-methyldopamine[side 1]
ADP + phosphate + 5-(glutathion-S-yl)-N-methyl-alpha-methyldopamine[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + 5-chloro-methyl fluorescein diacetate[side 1]
ADP + phosphate + 5-chloro-methyl fluorescein diacetate[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + arsenic triglutathione[side 1]
ADP + phosphate + arsenic triglutathione[side 2]
show the reaction diagram
ATP + H2O + Bi3+-glutathione[side 1]
ADP + phosphate + Bi3+-glutathione[side 2]
show the reaction diagram
-
-
-
-
?
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
show the reaction diagram
ATP + H2O + glutathione disulfide[side 1]
ADP + phosphate + glutathione disulfide[side 2]
show the reaction diagram
ATP + H2O + glutathione-S-conjugate[side 1]
ADP + phosphate + glutathione-S-conjugate[side 2]
show the reaction diagram
ATP + H2O + glutathione-S-conjugate[side 1] + leukotriene C4[side 1]
ADP + phosphate + glutathione-S-conjugate[side 2] + leukotriene C4[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + glutathione[side 1] + vincristine[side 1]
ADP + phosphate + glutathione[side 2] + vincristine[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + GSSG[side 1]
ADP + phosphate + GSSG[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + leukotriene C4[side 1]
ADP + phosphate + leukotriene C4[side 2]
show the reaction diagram
ATP + H2O + menadione-glutathione[side 1]
ADP + phosphate + menadione-glutathione[side 2]
show the reaction diagram
menadione-glutathione is thiodione
-
-
?
ATP + H2O + MK571[side 1]
ADP + phosphate + MK571[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + monochlorobimane[side 1]
ADP + phosphate + monochlorobimane[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(1-chloro-2,4-dinitrobenzyl)-glutathione[side 1]
ADP + phosphate + S-(1-chloro-2,4-dinitrobenzyl)-glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(15-deoxy-D12,14-prostaglandin J2)glutathione[side 1]
ADP + phosphate + S-(15-deoxy-D12,14-prostaglandin J2)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(15-deoxy-DELTA12,14-prostaglandin J2)glutathione[side 1]
ADP + phosphate + S-(15-deoxy-DELTA12,14-prostaglandin J2)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(17beta-estradiol)glutathione[side 1]
ADP + phosphate + S-(17beta-estradiol)glutathione[side 2]
show the reaction diagram
substrate for isoform MRP4
-
-
?
ATP + H2O + S-(17beta-glucuronosyl estradiol)glutathione[side 1]
ADP + phosphate + S-(17beta-glucuronosyl estradiol)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(2,4-dinitrophenyl)glutathione[side 1]
ADP + phosphate + S-(2,4-dinitrophenyl)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(4-(methylnitrosamino)-1-(3-pyridyl)1-1-butanol-glucuronidyl)glutathione[side 1]
ADP + phosphate + S-(4-(methylnitrosamino)-1-(3-pyridyl)1-1-butanol-glucuronidyl)glutathione[side 2]
show the reaction diagram
substrate for isoform MRP1
-
-
?
ATP + H2O + S-(4-hydroxy-nonenal)glutathione[side 1]
ADP + phosphate + S-(4-hydroxy-nonenal)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(4-hydroxynonenal)glutathione[side 1]
ADP + phosphate + S-(4-hydroxynonenal)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(6-mercaptopurinyl)glutathione[side 1]
ADP + phosphate + S-(6-mercaptopurinyl)glutathione[side 2]
show the reaction diagram
substrate for isoforms MRP4 and MRP5
-
-
?
ATP + H2O + S-(6-thioguaninyl)glutathione[side 1]
ADP + phosphate + S-(6-thioguaninyl)glutathione[side 2]
show the reaction diagram
substrate for isoforms MRP4 and MRP5
-
-
?
ATP + H2O + S-(6alpha-glucuronosyl hyodeoxycholate)glutathione[side 1]
ADP + phosphate + S-(6alpha-glucuronosyl hyodeoxycholate)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(acetaminophen)glutathione[side 1]
ADP + phosphate + S-(acetaminophen)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(aflatoxin B1 epoxidyl)glutathione[side 1]
ADP + phosphate + S-(aflatoxin B1 epoxidyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(aflatoxin B1)glutathione[side 1]
ADP + phosphate + S-(aflatoxin B1)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(arsenic)glutathione[side 1]
ADP + phosphate + S-(arsenic)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(arsenite)glutathione[side 1]
ADP + phosphate + S-(arsenite)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(atrazinyl)glutathione[side 1]
ADP + phosphate + S-(atrazinyl)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(bilirubin glucuronide)glutathione[side 1]
ADP + phosphate + S-(bilirubin glucuronide)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(bimanyl)glutathione[side 1]
ADP + phosphate + S-(bimanyl)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(C4-glutathione)glutathione[side 1]
ADP + phosphate + S-(C4-glutathione)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(calcein acetoxymethyl ester)glutathione[side 1]
ADP + phosphate + S-(calcein acetoxymethyl ester)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(calcein-AM)glutathione[side 1]
ADP + phosphate + S-(calcein-AM)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(cAMP)glutathione[side 1]
ADP + phosphate + S-(cAMP)glutathione[side 2]
show the reaction diagram
substrate for isoform MRP4
-
-
?
ATP + H2O + S-(chelerythrinyl)glutathione[side 1]
ADP + phosphate + S-(chelerythrinyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(chlorambucil)glutathione[side 1]
ADP + phosphate + S-(chlorambucil)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(chlorambucilyl)glutathione[side 1]
ADP + phosphate + S-(chlorambucilyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(cholyl)glutathione[side 1]
ADP + phosphate + S-(cholyl)glutathione[side 2]
show the reaction diagram
substrate for isoform MRP4
-
-
?
ATP + H2O + S-(curcuminyl)glutathione[side 1]
ADP + phosphate + S-(curcuminyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(cyclophosphamidyl)glutathione[side 1]
ADP + phosphate + S-(cyclophosphamidyl)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(daunorubicin)glutathione[side 1]
ADP + phosphate + S-(daunorubicin)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(daunorubicinyl)glutathione[side 1]
ADP + phosphate + S-(daunorubicinyl)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(deoxyprostaglandin J2)glutathione[side 1]
ADP + phosphate + S-(deoxyprostaglandin J2)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(doxorubicinyl)glutathione[side 1]
ADP + phosphate + S-(doxorubicinyl)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(estrone 3-sulfate)glutathione[side 1]
ADP + phosphate + S-(estrone 3-sulfate)glutathione[side 2]
show the reaction diagram
substrate for isoform MRP1
-
-
?
ATP + H2O + S-(estrone-3-sulfyl)glutathione[side 1]
ADP + phosphate + S-(estrone-3-sulfyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(ethacrynic acid)glutathione[side 1]
ADP + phosphate + S-(ethacrynic acid)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(etoposidyl)glutathione[side 1]
ADP + phosphate + S-(etoposidyl)glutathione[side 2]
show the reaction diagram
substrate for isoforms MRP1 and MRP2
-
-
?
ATP + H2O + S-(glycocholyl)glutathione[side 1]
ADP + phosphate + S-(glycocholyl)glutathione[side 2]
show the reaction diagram
substrate for isoform MRP4
-
-
?
ATP + H2O + S-(hydroxynonenyl)glutathione[side 1]
ADP + phosphate + S-(hydroxynonenyl)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(leukotriene C4)glutathione[side 1]
ADP + phosphate + S-(leukotriene C4)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(melphalan)glutathione[side 1]
ADP + phosphate + S-(melphalan)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(melphalanyl)glutathione[side 1]
ADP + phosphate + S-(melphalanyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(methoxychloro)glutathione[side 1]
ADP + phosphate + S-(methoxychloro)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(methylfluorescinyl)glutathione[side 1]
ADP + phosphate + S-(methylfluorescinyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(methylmercury)glutathione[side 1]
ADP + phosphate + S-(methylmercury)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(metolachloro)glutathione[side 1]
ADP + phosphate + S-(metolachloro)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(mitoxantronyl)glutathione[side 1]
ADP + phosphate + S-(mitoxantronyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(N-ethylmaleimidyl)glutathione[side 1]
ADP + phosphate + S-(N-ethylmaleimidyl)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(prostaglandin A2)glutathione[side 1]
ADP + phosphate + S-(prostaglandin A2)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-(prostaglandin E1)glutathione[side 1]
ADP + phosphate + S-(prostaglandin E1)glutathione[side 2]
show the reaction diagram
substrate for isoform MRP4
-
-
?
ATP + H2O + S-(prostaglandin E2)glutathione[side 1]
ADP + phosphate + S-(prostaglandin E2)glutathione[side 2]
show the reaction diagram
substrate for isoform MRP4
-
-
?
ATP + H2O + S-(sestamibi)glutathione[side 1]
ADP + phosphate + S-(sestamibi)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(sulfobromophthaleinyl)glutathione[side 1]
ADP + phosphate + S-(sulfobromophthaleinyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(sulforanyl)glutathione[side 1]
ADP + phosphate + S-(sulforanyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(sulforaphanyl)glutathione[side 1]
ADP + phosphate + S-(sulforaphanyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(taurocholyl)glutathione[side 1]
ADP + phosphate + S-(taurocholyl)glutathione[side 2]
show the reaction diagram
substrate for isoform MRP4
-
-
?
ATP + H2O + S-(tetrofosmin)glutathione[side 1]
ADP + phosphate + S-(tetrofosmin)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(thiotepa)glutathione[side 1]
ADP + phosphate + S-(thiotepa)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(thiotepyl)glutathione[side 1]
ADP + phosphate + S-(thiotepyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(vinblastinyl)glutathione[side 1]
ADP + phosphate + S-(vinblastinyl)glutathione[side 2]
show the reaction diagram
substrate for isoforms MRP1 and MRP2
-
-
?
ATP + H2O + S-(vincristinyl)glutathione[side 1]
ADP + phosphate + S-(vincristinyl)glutathione[side 2]
show the reaction diagram
ATP + H2O + S-decylglutathione[side 1]
ADP + phosphate + S-decylglutathione[side 2]
show the reaction diagram
ATP + H2O + S-ethylglutathione[side 1]
ADP + phosphate + S-ethylglutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-glutathionyl-conjugated 3'-(3-methoxymorpholino)doxorubicin[side 1]
ADP + phosphate + S-glutathionyl-conjugated 3'-(3-methoxymorpholino)doxorubicin[side 2]
show the reaction diagram
about 123% activity
-
-
?
ATP + H2O + S-glutathionyl-doxorubicin[side 1]
ADP + phosphate + S-glutathionyl-doxorubicin[side 2]
show the reaction diagram
about 125% activity
-
-
?
ATP + H2O + S-hexylglutathione[side 1]
ADP + phosphate + S-hexylglutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-methylglutathione[side 1]
ADP + phosphate + S-methylglutathione[side 2]
show the reaction diagram
ATP + H2O + S-metolachloroglutathione[side 1]
ADP + phosphate + S-metolachloroglutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-nitrosoglutathione[side 1]
ADP + phosphate + S-nitrosoglutathione[side 2]
show the reaction diagram
O95255, P33527, Q15439, Q15440, Q92887
-
-
-
?
ATP + H2O + S-octylglutathione[side 1]
ADP + phosphate + S-octylglutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + sulforaphane-S-glutathione[side 1]
ADP + phosphate + sulforaphane-S-glutathione[side 2]
show the reaction diagram
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + H2O + glutathione-S-conjugate[side 1]
ADP + phosphate + glutathione-S-conjugate[side 2]
show the reaction diagram
ATP + H2O + leukotriene C4[side 1]
ADP + phosphate + leukotriene C4[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + Bi3+-glutathione[side 1]
ADP + phosphate + Bi3+-glutathione[side 2]
show the reaction diagram
-
-
-
-
?
ATP + H2O + glutathione disulfide[side 1]
ADP + phosphate + glutathione disulfide[side 2]
show the reaction diagram
O95255, P33527, Q15439, Q15440, Q92887
-
-
-
?
ATP + H2O + glutathione-S-conjugate[side 1]
ADP + phosphate + glutathione-S-conjugate[side 2]
show the reaction diagram
ATP + H2O + glutathione-S-conjugate[side 1] + leukotriene C4[side 1]
ADP + phosphate + glutathione-S-conjugate[side 2] + leukotriene C4[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + leukotriene C4[side 1]
ADP + phosphate + leukotriene C4[side 2]
show the reaction diagram
ATP + H2O + menadione-glutathione[side 1]
ADP + phosphate + menadione-glutathione[side 2]
show the reaction diagram
menadione-glutathione is thiodione
-
-
?
ATP + H2O + S-(15-deoxy-DELTA12,14-prostaglandin J2)glutathione[side 1]
ADP + phosphate + S-(15-deoxy-DELTA12,14-prostaglandin J2)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(calcein-AM)glutathione[side 1]
ADP + phosphate + S-(calcein-AM)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(hydroxynonenyl)glutathione[side 1]
ADP + phosphate + S-(hydroxynonenyl)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(leukotriene C4)glutathione[side 1]
ADP + phosphate + S-(leukotriene C4)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-(prostaglandin A2)glutathione[side 1]
ADP + phosphate + S-(prostaglandin A2)glutathione[side 2]
show the reaction diagram
-
-
-
?
ATP + H2O + S-nitrosoglutathione[side 1]
ADP + phosphate + S-nitrosoglutathione[side 2]
show the reaction diagram
O95255, P33527, Q15439, Q15440, Q92887
-
-
-
?
ATP + H2O + sulforaphane-S-glutathione[side 1]
ADP + phosphate + sulforaphane-S-glutathione[side 2]
show the reaction diagram
-
-
-
?
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mg2+
100% activity in the presence of 2 mM Mg2+
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
4-[4-(2-phenylethyl)piperazin-1-yl]-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile
complete inhibition at 10 nM
cyclosporin
-
cyclosporine A
-
Decanol
decanol causes a small, but significant and concentration-dependent (0.1-1.0 mM) inhibition of the ATPase activity
dipyridamole
-
doxorubicin
-
EDTA
complete inhibition at 2 mM
glibenclamide
-
leukotriene C4
-
MK571
N-ethylmaleimide
-
orthovanadate
the ATPase activity of GST-tagged nucleotide-binding domains 1 and 2 is inhibited more than 40% by 2 mM orthovanadate
QCRL-4
monoclonal antibody
-
Sodium azide
the ATPase activity of GST-tagged nucleotide-binding domains 1 and 2 is inhibited more than 70% by 2 mM sodium azide
sodium orthovanadate
verapamil
additional information
N-ethylmaleimide does not significantly inhibit the ATPase activities at concentrations of up to 2 mM
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
4,5-bis(benzylamino)-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile
about 15% increase of activity at 10 nM
4-(benzylamino)-5-[(3-phenylpropyl)amino]-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile
about 15% increase of activity at 10 nM
4-(benzylamino)-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile
-
4-anilino-5-(benzylamino)-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile
15% increase of activity at 10 nM
4-anilino-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile
-
4-[(2-phenylethyl)amino]-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile
-
4-[(3-phenylpropyl)amino]-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile
-
5-(2-phenylethyl)-4-[(2-phenylethyl)amino]-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile
about 20% increase of activity at 10 nM
5-(2-phenylethyl)-4-[(3-phenylpropyl)amino]-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile
about 20% increase of activity at 10 nM
5-(benzylamino)-4-(methylamino)-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile
about 10% increase of activity at 10 nM
6-(4-benzylpiperazin-1-yl)-7H-purine
about 20% increase of activity at 10 nM
6-(4-phenylpiperazin-1-yl)-7H-purine
about 7% increase of activity at 10 nM
6-[4-(2-phenylethyl)piperazin-1-yl]-7H-purine
about 7% increase of activity at 10 nM
6-[4-(diphenylmethyl)piperazin-1-yl]-7H-purine
25% increase of activity at 10 nM
decyl-maltoside
1.0 mM decyl-maltoside is able to stimulate the ATPase activities of the isolated nucleotide-binding domains more than 2fold
glutathione
S-decylglutathione
0.2-0.25 mM S-decylglutathione is able to stimulate the ATPase activities of the isolated nucleotide-binding domains more than 2fold
S-Methylglutathione
-
-
verapamil
-
vincristine
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0095
4-(glutathione-S-yl)-quinoline-1-oxide[side 1]
-
pH and temperature not specified in the publication
0.00032
arsenic triglutathione[side 1]
at pH 7.5 and 37°C
0.34 - 0.91
ATP
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0028
antimonite
at pH 7.5 and 37°C
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0004
MK571
Homo sapiens
with S-(daunorubicinyl)glutathione as substrate, at pH 7.4 and 37°C
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
UniProt
Manually annotated by BRENDA team
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
O95255, P33527, Q15439, Q15440, Q92887
-
Manually annotated by BRENDA team
O95255, P33527, Q15439, Q15440, Q92887
-
Manually annotated by BRENDA team
O95255, P33527, Q15439, Q15440, Q92887
-
Manually annotated by BRENDA team
O95255, P33527, Q15439, Q15440, Q92887
-
Manually annotated by BRENDA team
O95255, P33527, Q15439, Q15440, Q92887
-
Manually annotated by BRENDA team
O95255, P33527, Q15439, Q15440, Q92887
-
Manually annotated by BRENDA team
O95255, P33527, Q15439, Q15440, Q92887
-
Manually annotated by BRENDA team
O95255, P33527, Q15439, Q15440, Q92887
-
Manually annotated by BRENDA team
O95255, P33527, Q15439, Q15440, Q92887
-
Manually annotated by BRENDA team
O95255, P33527, Q15439, Q15440, Q92887
-
Manually annotated by BRENDA team
additional information
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
the enzyme plays an essential role in detoxification and defense against oxidative stress
metabolism
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
MRP5_HUMAN
1437
11
160660
Swiss-Prot
-
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
190000
gel filtration
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
glutathione-Sepharose column chromatography
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in BHK-21 cells
expressed in Escherichia coli DH5alpha cells
expressed in Sf9 insect cells
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Sharma, R.; Singhal, S.; Cheng, J.; Yang, Y.; Sharma, A.; Zimniak, P.; Awasthi, S.; Awasthi, Y.
RLIP76 is the major ATP-dependent transporter of glutathione-conjugates and doxorubicin in human erythrocytes
Arch. Biochem. Biophys.
391
171-179
2001
Homo sapiens (Q15311), Homo sapiens
Manually annotated by BRENDA team
Hessel, S.; John, A.; Seidel, A.; Lampen, A.
Multidrug resistance-associated proteins are involved in the transport of the glutathione conjugates of the ultimate carcinogen of benzo[a]pyrene in human Caco-2 cells
Arch. Toxicol.
87
269-280
2013
Homo sapiens (O15438), Homo sapiens (P33527), Homo sapiens (Q92887), Homo sapiens (Q9UNQ0)
Manually annotated by BRENDA team
Zhang, Y.; Callaway, E.
High cellular accumulation of sulphoraphane, a dietary anticarcinogen, is followed by rapid transporter-mediated export as a glutathione conjugate
Biochem. J.
364
301-307
2002
Homo sapiens (Q8HXQ5), Homo sapiens
Manually annotated by BRENDA team
Karwatsky, J.; Daoud, R.; Cai, J.; Gros, P.; Georges, E.
Binding of a photoaffinity analogue of glutathione to MRP1 (ABCC1) within two cytoplasmic regions (L0 and L1) as well as transmembrane domains 10-11 and 16-17
Biochemistry
42
3286-3294
2003
Homo sapiens (P33527)
Manually annotated by BRENDA team
Peklak-Scott, C.; Townsend, A.; Morrow, C.
Dynamics of glutathione conjugation and conjugate efflux in detoxification of the carcinogen, 4-nitroquinoline 1-oxide Contributions of glutathione, glutathione S-transferase, and MRP1
Biochemistry
44
4426-4433
2005
Homo sapiens
Manually annotated by BRENDA team
Schmitt, S.M.; Stefan, K.; Wiese, M.
Pyrrolopyrimidine derivatives and purine analogs as novel activators of multidrug resistance-associated protein 1 (MRP1, ABCC1)
Biochim. Biophys. Acta
1859
69-79
2017
Homo sapiens (P33527), Canis lupus familiaris (Q6UR05)
Manually annotated by BRENDA team
Homolya, L.; Varadi, A.; Sarkadi, B.
Multidrug resistance-associated proteins Export pumps for conjugates with glutathione, glucuronate or sulfate
Biofactors
17
103-114
2003
Homo sapiens (O15439), Homo sapiens (O15440), Homo sapiens (O95255), Homo sapiens (P33527), Homo sapiens (Q92887)
Manually annotated by BRENDA team
Keppler, D.; Leier, I.; Jedlitschky, G.
Transport of glutathione conjugates and glucuronides by the multidrug resistance proteins MRP1 and MRP2
Biol. Chem.
378
787-791
1997
Homo sapiens (Q92887), Homo sapiens
Manually annotated by BRENDA team
Renes, J.; De Vries, E.; Nienhuis, E.; Jansen, P.; Mueller, M.
ATP- and glutathione-dependent transport of chemotherapeutic drugs by the multidrug resistance protein MRP1
Br. J. Pharmacol.
126
681-688
1999
Homo sapiens (P33527)
Manually annotated by BRENDA team
Awasthi, Y.; Singhal, S.; Zimniak, P.; Piper, J.; Pikula, S.; Bandorowicz-Pikula, J.; Lin, J.; Srivastava, S.; Singh, S.; Awasthi, S.
Glutathione-linked pathways in drug resistance Characterization and functional reconstitution of human erythrocyte glutathione-conjugate transporter
Clin. Chem. Enzymol. Commun.
8
431-448
1999
Homo sapiens
-
Manually annotated by BRENDA team
Vaidya, S.; Walsh, S.; Gerk, P.
Application of human placental villous tissue explants to study ABC transporter mediated efflux of 2,4-dinitrophenyl-S-glutathione
Curr. Pharm. Biotechnol.
12
814-823
2011
Homo sapiens (Q92887), Homo sapiens
Manually annotated by BRENDA team
Cool, R.; Veenstra, M.; Van Klompenburg, W.; Heyne, R.; Mueller, M.; De Vries, E.; Van Veen, H.; Konings, W.
S-decyl-glutathione nonspecifically stimulates the ATPase activity of the nucleotide-binding domains of the human multidrug resistance-associated protein, MRP1 (ABCC1)
Eur. J. Biochem.
269
3470-3478
2002
Homo sapiens (P33527)
-
Manually annotated by BRENDA team
Zamek-Gliszczynski, M.; Hoffmaster, K.; Nezasa, K.; Tallman, M.; Brouwer, K.
Integration of hepatic drug transporters and phase II metabolizing enzymes Mechanisms of hepatic excretion of sulfate, glucuronide, and glutathione metabolites
Eur. J. Pharm. Sci.
27
447-486
2006
Mus musculus, Mus musculus (P04095), Mus musculus (Q7TMS5), Mus musculus (Q8VI47), Homo sapiens (O15438), Homo sapiens (O15439), Homo sapiens (Q92887), Homo sapiens (Q9UNQ0), Rattus norvegicus (Q63120), Rattus norvegicus (Q6QMG6), Rattus norvegicus (Q80W57), Rattus norvegicus (Q88563)
Manually annotated by BRENDA team
Deeley, R.; Cole, S.
Substrate recognition and transport by multidrug resistance protein 1 (ABCC1)
FEBS Lett.
580
1103-1111
2006
Homo sapiens (P08183)
Manually annotated by BRENDA team
Fallatah, O.; Georges, E.
Apigenin-induced ABCC1-mediated efflux of glutathione from mature erythrocytes inhibits the proliferation of Plasmodium falciparum
Int. J. Antimicrob. Agents
50
673-677
2017
Homo sapiens (P08183)
Manually annotated by BRENDA team
Van Luyn, M.; Muller, M.; Renes, J.; Meijer, C.; Scheper, R.; Nienhuis, E.; Mulder, N.; Jansen, P.; De Vries, E.
Transport of glutathione conjugates into secretory vesicles is mediated by the multidrug-resistance protein 1
Int. J. Cancer
76
55-62
1998
Homo sapiens (P33527), Homo sapiens
Manually annotated by BRENDA team
Manciu, L.; Chang, X.; Buyse, F.; Hou, Y.; Gustot, A.; Riordani, J.; Ruysschaert, J.
Intermediate structural states involved in MRP1-mediated drug transport. Role of glutathione
J. Biol. Chem.
278
3347-3356
2003
Homo sapiens (P33527)
Manually annotated by BRENDA team
Leslie, E.; Haimeur, A.; Waalkes, M.
Arsenic transport by the human multidrug resistance protein 1 (MRP1/ABCC1) Evidence that a tri-glutathione conjugate is required
J. Biol. Chem.
279
32700-32708
2004
Homo sapiens (P33527), Homo sapiens (Q92887)
Manually annotated by BRENDA team
Cole, S.
Multidrug resistance protein 1 (MRP1, ABCC1), a multitasking ATP-binding cassette (ABC,) transporter
J. Biol. Chem.
289
30880-30888
2014
Homo sapiens (P33527)
Manually annotated by BRENDA team
Ballatori, N.; Krance, S.; Marchan, R.; Hammond, C.
Plasma membrane glutathione transporters and their roles in cell physiology and pathophysiology
Mol. Aspects Med.
30
13-28
2009
Homo sapiens, Homo sapiens (O95255), Homo sapiens (P33527), Homo sapiens (Q15439), Homo sapiens (Q15440), Homo sapiens (Q92887)
Manually annotated by BRENDA team
Vaidya, S.; Walsh, S.; Gerk, P.
Formation and efflux of ATP-binding cassette transporter substrate 2,4-dinitrophenyl-S-glutathione from cultured human term placental villous tissue fragments
Mol. Pharm.
6
1689-1702
2009
Homo sapiens (P33527), Homo sapiens (Q92887)
Manually annotated by BRENDA team
Morrow, C.; Peklak-Scott, C.; Bishwokarma, B.; Kute, T.; Smitherman, P.; Townsend, A.
Multidrug resistance protein 1 (MRP1, ABCC1) mediates resistance to mitoxantrone via glutathione-dependent drug efflux
Mol. Pharmacol.
69
1499-1505
2006
Homo sapiens (P33527)
Manually annotated by BRENDA team
Koley, D.; Bard, A.
Inhibition of the MRP1-mediated transport of the menadione-glutathione conjugate (thiodione) in HeLa cells as studied by SECM
Proc. Natl. Acad. Sci. USA
109
11522-11527
2012
Homo sapiens (P33527)
Manually annotated by BRENDA team
Hong, Y.; Lai, Y.; Chan, G.; Sun, H.
Glutathione and multidrug resistance protein transporter mediate a self-propelled disposal of bismuth in human cells
Proc. Natl. Acad. Sci. USA
112
3211-3216
2015
Homo sapiens
Manually annotated by BRENDA team
Ballatori, N.; Hammond, C.; Cunningham, J.; Krance, S.; Marchan, R.
Molecular mechanisms of reduced glutathione transport Role of the MRP/CFTR/ABCC and OATP/SLC21A families of membrane proteins
Toxicol. Appl. Pharmacol.
204
238-255
2005
Saccharomyces cerevisiae, Rattus norvegicus, Homo sapiens (O15439), Homo sapiens (O15440), Homo sapiens (P33527), Homo sapiens (Q92887), Homo sapiens
Manually annotated by BRENDA team
Cole, S.; Deeley, R.
Transport of glutathione and glutathione conjugates by MRP1
Trends Pharmacol. Sci.
27
438-446
2006
Homo sapiens (P33527)
Manually annotated by BRENDA team