Proteins > Broad substrate specificity ATP-binding cassette transporter ABCG2
Page last updated: 2024-08-07 18:53:26

Broad substrate specificity ATP-binding cassette transporter ABCG2

A broad substrate specificity ATP-binding cassette transporter ABCG2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9UNQ0]

Synonyms

EC 7.6.2.2;
ATP-binding cassette sub-family G member 2;
Breast cancer resistance protein;
CDw338;
Mitoxantrone resistance-associated protein;
Placenta-specific ATP-binding cassette transporter;
Urate exporter

Research

Bioassay Publications (72)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's16 (22.22)29.6817
2010's44 (61.11)24.3611
2020's12 (16.67)2.80

Compounds (151)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
b 844-39Homo sapiens (human)IC506.100011
benzbromaroneHomo sapiens (human)IC500.200011
beta-naphthoflavoneHomo sapiens (human)IC507.185022
caffeineHomo sapiens (human)IC5014,000.000011
verapamilHomo sapiens (human)IC50192.000133
candesartan cilexetilHomo sapiens (human)IC505.000011
cl 387785Homo sapiens (human)IC500.200011
clofazimineHomo sapiens (human)IC503.200011
dipyridamoleHomo sapiens (human)IC506.400011
fenofibrateHomo sapiens (human)IC505.100011
furosemideHomo sapiens (human)IC503.200011
glyburideHomo sapiens (human)IC50150.000022
itraconazoleHomo sapiens (human)IC502.000011
lansoprazoleHomo sapiens (human)IC5014.400011
losartanHomo sapiens (human)IC5035.000011
mitoxantroneHomo sapiens (human)IC500.903811
nicardipineHomo sapiens (human)IC5010.698022
nifedipineHomo sapiens (human)IC5050.500011
nimodipineHomo sapiens (human)IC5013.700011
nitrendipineHomo sapiens (human)IC5021.100011
omeprazoleHomo sapiens (human)IC5017.600011
pantoprazoleHomo sapiens (human)IC507.750022
pd 153035Homo sapiens (human)IC502.025022
rabeprazoleHomo sapiens (human)IC508.500011
imatinibHomo sapiens (human)IC502.909666
sulfasalazineHomo sapiens (human)IC500.460011
thioridazineHomo sapiens (human)IC506.600011
delavirdineHomo sapiens (human)IC5018.700011
reserpineHomo sapiens (human)IC5016.900933
estroneHomo sapiens (human)IC506.500022
1,3-benzodioxoleHomo sapiens (human)IC500.940011
flavoneHomo sapiens (human)IC5021.500022
alpha-naphthoflavoneHomo sapiens (human)IC501.355022
diltiazemHomo sapiens (human)IC50851.138011
mefloquineHomo sapiens (human)IC5018.000011
topotecanHomo sapiens (human)IC500.170011
atorvastatinHomo sapiens (human)IC504.300011
efavirenzHomo sapiens (human)IC5020.600011
nelfinavirHomo sapiens (human)IC5012.500022
amprenavirHomo sapiens (human)IC50181.000011
telmisartanHomo sapiens (human)IC5016.900011
tangeretinHomo sapiens (human)IC5018.000022
nobiletinHomo sapiens (human)IC504.650022
vexibinolHomo sapiens (human)IC502.205022
pinostrobinHomo sapiens (human)IC5019.950022
atovaquoneHomo sapiens (human)IC500.230011
5,7-dimethoxyflavoneHomo sapiens (human)IC5010.100022
lopinavirHomo sapiens (human)IC507.600011
3,5,7,3',4'-pentamethoxyflavoneHomo sapiens (human)IC501.351022
6-methoxyflavanoneHomo sapiens (human)IC5032.500022
sn 38Homo sapiens (human)IC500.176011
elacridarHomo sapiens (human)IC500.285277
gefitinibHomo sapiens (human)IC501.290055
febuxostatHomo sapiens (human)IC500.027011
sinensetinHomo sapiens (human)IC508.650022
3-methoxyflavoneHomo sapiens (human)IC501.245022
6-methoxyflavoneHomo sapiens (human)IC506.700022
atazanavirHomo sapiens (human)IC5069.100011
tariquidarHomo sapiens (human)IC501.23631212
3,3',4',5,6,7,8-heptamethoxyflavoneHomo sapiens (human)IC501.500022
erlotinibHomo sapiens (human)IC5025.065022
scutellarinHomo sapiens (human)IC5010.000011
etravirineHomo sapiens (human)IC506.000011
lapatinibHomo sapiens (human)IC503.200011
sorafenibHomo sapiens (human)IC503.100011
3',4'-dimethoxy-alpha-naphthoflavoneHomo sapiens (human)IC501.180022
5-Hydroxy-7-methoxy-6-methylflavoneHomo sapiens (human)IC502.900022
5,7-dimethoxy-2-phenyl-3,4-dihydro-2H-1-benzopyran-4-oneHomo sapiens (human)IC5024.500022
ritonavirHomo sapiens (human)IC5019.500011
tryptoquivalineHomo sapiens (human)IC501.58991212
tryptoquivalineHomo sapiens (human)Ki1.300011
1-methoxy-10H-acridin-9-oneHomo sapiens (human)IC506.300011
saquinavirHomo sapiens (human)IC5019.500022
abacavirHomo sapiens (human)IC50385.000011
6-prenylchrysinHomo sapiens (human)IC500.290022
tacrolimusHomo sapiens (human)IC503.300011
diethylstilbestrolHomo sapiens (human)IC500.500022
ketoconazoleHomo sapiens (human)IC5015.300011
posaconazoleHomo sapiens (human)IC506.000011
micafunginHomo sapiens (human)IC5021.000011
8-prenylnaringeninHomo sapiens (human)IC503.100011
s 1033Homo sapiens (human)IC502.500011
N-[3-(trifluoromethyl)phenyl]-4-quinazolinamineHomo sapiens (human)IC501.245022
diethylstilbestrol dipropionateHomo sapiens (human)IC503.000022
chlorprothixeneHomo sapiens (human)IC5042.000011
curcuminHomo sapiens (human)IC501.630011
N-{3-[(2-phenylquinazolin-4-yl)amino]phenyl}acetamideHomo sapiens (human)IC500.251022
cancidasHomo sapiens (human)IC506.000011
fusidic acidHomo sapiens (human)IC5052.000011
dasatinibHomo sapiens (human)IC502.000011
zd 6474Homo sapiens (human)IC500.200011
sq 109Homo sapiens (human)IC505.500011
quercetinHomo sapiens (human)IC507.250022
apigeninHomo sapiens (human)IC508.333333
luteolinHomo sapiens (human)IC508.900011
ayaninHomo sapiens (human)IC502.280033
kaempferolHomo sapiens (human)IC505.450022
harmineHomo sapiens (human)GI501.670033
harmineHomo sapiens (human)IC505.080011
genisteinHomo sapiens (human)IC507.850022
amphotericin bHomo sapiens (human)IC50127.000011
chrysinHomo sapiens (human)IC502.050022
morinHomo sapiens (human)IC5035.000022
pachypodolHomo sapiens (human)IC5017.200011
l 660,711Homo sapiens (human)IC5050.000011
tectochrysinHomo sapiens (human)IC503.000011
cyclosporineHomo sapiens (human)IC5024.654633
cyclosporineHomo sapiens (human)Ki0.500011
sirolimusHomo sapiens (human)IC501.900011
topiroxostatHomo sapiens (human)IC500.180011
licochalcone aHomo sapiens (human)IC502.27172424
5,4'-dihydroxy-3,6,7-trimethoxyflavoneHomo sapiens (human)IC501.600022
bosutinibHomo sapiens (human)IC502.000011
su 11248Homo sapiens (human)IC503.000011
5-hydroxy-3,3',4',7-tetramethoxyflavoneHomo sapiens (human)IC500.600044
flavokawain aHomo sapiens (human)IC504.415022
Isoliquiritigenin 4,4'-dimethyl etherHomo sapiens (human)IC503.200022
3,3',4,5'-tetramethoxy-trans-stilbeneHomo sapiens (human)IC500.160022
2-chloro-4',6'-dimethoxy-2'-hydroxychalconeHomo sapiens (human)IC504.045022
metochalconeHomo sapiens (human)IC502.125022
proguanilHomo sapiens (human)IC50118.000011
rilpivirineHomo sapiens (human)IC501.500011
sophoraflavanone aHomo sapiens (human)IC5012.300011
isavuconazoleHomo sapiens (human)IC5011.000011
timcodarHomo sapiens (human)IC50100.000011
tivozanibHomo sapiens (human)IC500.070011
ko 143Homo sapiens (human)GI500.540333
ko 143Homo sapiens (human)IC500.18824141
regorafenibHomo sapiens (human)IC503.000011
alisporivirHomo sapiens (human)IC502.500011
fostamatinibHomo sapiens (human)IC500.050011
wk-x-34Homo sapiens (human)IC501.293133
xr 9577Homo sapiens (human)IC500.75161111
gdc 0449Homo sapiens (human)IC501.400011
bms 754807Homo sapiens (human)IC5010.200011
ponatinibHomo sapiens (human)IC500.040011
cobicistatHomo sapiens (human)IC5059.000011
gs-9451Homo sapiens (human)IC501.400011
alectinibHomo sapiens (human)IC501.500011
novobiocinHomo sapiens (human)IC5061.393955
dolutegravirHomo sapiens (human)IC5048.500022
chir 258Homo sapiens (human)IC5010.300011
rifampinHomo sapiens (human)IC5056.000011
tmc 256c1Homo sapiens (human)IC5012.800011
amg531Homo sapiens (human)IC503.100011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
verapamilHomo sapiens (human)EC5019.100022
whi p154Homo sapiens (human)EC500.189011
pargylineHomo sapiens (human)EC501.000011
gefitinibHomo sapiens (human)EC500.300011
tariquidarHomo sapiens (human)EC500.055022
erlotinibHomo sapiens (human)EC500.170011
lapatinibHomo sapiens (human)EC503.200011
tryptoquivalineHomo sapiens (human)EC501.000011
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamideHomo sapiens (human)EC501.420011
quercetinHomo sapiens (human)EC500.195333
cyclosporineHomo sapiens (human)EC501.750011
licochalcone aHomo sapiens (human)EC5014.000011
ko 143Homo sapiens (human)EC500.03981010
osi 906Homo sapiens (human)EC500.104011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
mitoxantroneHomo sapiens (human)Kact7.000011
prazosinHomo sapiens (human)Kact1.000011
daunorubicinHomo sapiens (human)Kact2.500011
4-methylumbelliferyl sulfateHomo sapiens (human)Km13.000011
sn 38Homo sapiens (human)Km4.000011
methotrexateHomo sapiens (human)Km2,560.000033
estrone sulfateHomo sapiens (human)Km11.900022
rhodamine 123Homo sapiens (human)Kact4.500011

Enables

This protein enables 14 target(s):

TargetCategoryDefinition
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
ATP bindingmolecular functionBinding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
organic anion transmembrane transporter activitymolecular functionEnables the transfer of organic anions from one side of a membrane to the other. Organic anions are atoms or small molecules with a negative charge which contain carbon in covalent linkage. [GOC:ai]
ABC-type xenobiotic transporter activitymolecular functionCatalysis of the reaction: ATP + H2O + xenobiotic(in) = ADP + phosphate + xenobiotic(out). [EC:7.6.2.2]
urate transmembrane transporter activitymolecular functionEnables the transfer of urate from one side of a membrane to the other. Urate is the anion of uric acid, 2,6,8-trioxypurine, the end product of purine metabolism in certain mammals and the main excretory product in uricotelic animals. [GOC:ai]
biotin transmembrane transporter activitymolecular functionEnables the transfer of biotin from one side of a membrane to the other. Biotin is cis-tetrahydro-2-oxothieno(3,4-d)imidazoline-4-valeric acid; the (+) enantiomer is very widely distributed in cells and serves as a carrier in a number of enzymatic beta-carboxylation reactions. [GOC:ai]
efflux transmembrane transporter activitymolecular functionEnables the transfer of a specific substance or related group of substances from the inside of the cell to the outside of the cell across a membrane. [GOC:ai, GOC:mtg_transport, ISBN:0815340729]
ATP hydrolysis activitymolecular functionCatalysis of the reaction: ATP + H2O = ADP + H+ phosphate. ATP hydrolysis is used in some reactions as an energy source, for example to catalyze a reaction or drive transport against a concentration gradient. [RHEA:13065]
riboflavin transmembrane transporter activitymolecular functionEnables the transfer of riboflavin from one side of a membrane to the other. Riboflavin (vitamin B2) is a water-soluble B-complex vitamin, converted in the cell to FMN and FAD, cofactors required for the function of flavoproteins. [GOC:rn, PMID:16204239]
ATPase-coupled transmembrane transporter activitymolecular functionPrimary active transporter of a solute across a membrane, via the reaction: ATP + H2O = ADP + phosphate, to directly drive the transport of a substance across a membrane. The transport protein may be transiently phosphorylated (P-type transporters), or not (ABC-type transporters and other families of transporters). Primary active transport occurs up the solute's concentration gradient and is driven by a primary energy source. [GOC:mtg_transport, ISBN:0815340729]
identical protein bindingmolecular functionBinding to an identical protein or proteins. [GOC:jl]
protein homodimerization activitymolecular functionBinding to an identical protein to form a homodimer. [GOC:jl]
xenobiotic transmembrane transporter activitymolecular functionEnables the directed movement of a xenobiotic from one side of a membrane to the other. A xenobiotic is a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:go_curators, GOC:krc]
sphingolipid transporter activitymolecular functionEnables the directed movement of sphingolipids into, out of or within a cell, or between cells. Sphingolipids are a class of lipids containing the long-chain amine diol sphingosine or a closely related base (a sphingoid). [GOC:ai, ISBN:0198506732]

Located In

This protein is located in 7 target(s):

TargetCategoryDefinition
nucleoplasmcellular componentThat part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
apical plasma membranecellular componentThe region of the plasma membrane located at the apical end of the cell. [GOC:curators]
brush border membranecellular componentThe portion of the plasma membrane surrounding the brush border. [GOC:mah]
mitochondrial membranecellular componentEither of the lipid bilayers that surround the mitochondrion and form the mitochondrial envelope. [GOC:mah, NIF_Subcellular:sao1045389829]
membrane raftcellular componentAny of the small (10-200 nm), heterogeneous, highly dynamic, sterol- and sphingolipid-enriched membrane domains that compartmentalize cellular processes. Small rafts can sometimes be stabilized to form larger platforms through protein-protein and protein-lipid interactions. [PMID:16645198, PMID:20044567]
external side of apical plasma membranecellular componentThe leaflet the apical region of the plasma membrane that faces away from the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:ab, GOC:dos]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]

Involved In

This protein is involved in 14 target(s):

TargetCategoryDefinition
lipid transportbiological processThe directed movement of lipids into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Lipids are compounds soluble in an organic solvent but not, or sparingly, in an aqueous solvent. [ISBN:0198506732]
organic anion transportbiological processThe directed movement of organic anions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Organic anions are atoms or small molecules with a negative charge which contain carbon in covalent linkage. [GOC:ai, GOC:krc]
urate transportbiological processThe directed movement of urate into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:krc]
biotin transportbiological processThe directed movement of biotin into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Biotin is cis-tetrahydro-2-oxothieno(3,4-d)imidazoline-4-valeric acid; the (+) enantiomer is very widely distributed in cells and serves as a carrier in a number of enzymatic beta-carboxylation reactions. [GOC:ai]
sphingolipid biosynthetic processbiological processThe chemical reactions and pathways resulting in the formation of sphingolipids, any of a class of lipids containing the long-chain amine diol sphingosine or a closely related base (a sphingoid). [GOC:mah, ISBN:0198506732]
riboflavin transportbiological processThe directed movement of riboflavin into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Riboflavin (vitamin B2) is a water-soluble B-complex vitamin, converted in the cell to FMN and FAD, cofactors required for the function of flavoproteins. [GOC:rn, PMID:16204239]
urate metabolic processbiological processThe chemical reactions and pathways involving urate, the anion of uric acid, 2,6,8-trioxypurine, the end product of purine metabolism in certain mammals and the main excretory product in uricotelic animals. [ISBN:0198506732]
transmembrane transportbiological processThe process in which a solute is transported across a lipid bilayer, from one side of a membrane to the other. [GOC:dph, GOC:jid]
transepithelial transportbiological processThe directed movement of a substance from one side of an epithelium to the other. [GOC:mah, GOC:yaf, ISBN:0716731363]
renal urate salt excretionbiological processThe elimination of urate salt or uric acid from peritubular capillaries (or surrounding hemolymph in invertebrates) into the renal tubules to be incorporated subsequently into the urine. [GOC:jl, PMID:25287933, PMID:3906799, Wikipedia:Renal_physiology#Secretion]
export across plasma membranebiological processThe directed movement of some substance from inside of a cell, across the plasma membrane and into the extracellular region. [GOC:pg]
transport across blood-brain barrierbiological processThe directed movement of substances (e.g. macromolecules, small molecules, ions) through the blood-brain barrier. [GOC:aruk, GOC:bc, PMID:29377008]
cellular detoxificationbiological processAny process carried out at the cellular level that reduces or removes the toxicity of a toxic substance. These may include transport of the toxic substance away from sensitive areas and to compartments or complexes whose purpose is sequestration of the toxic substance. [GOC:vw]
xenobiotic transport across blood-brain barrierbiological processThe directed movement of a xenobiotic through the blood-brain barrier. [PMID:25053619]