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TargetDrug transporters

Broad substrate specificity ATP-binding cassette transporter ABCG2

SLC and ABC transporters governing uptake and efflux — distinct from the monoamine transporters.

Measurements
5
Compounds
1
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

ABCG2_HUMANABCG2Homo sapiens

Broad substrate specificity ATP-binding cassette transporter ABCG2

Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells11306452,12958161,19506252,20705604,28554189,30405239,31003562. Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme20705604,23189181. Also mediates the efflux of sphingosine-1-P from cells20110355. Acts as a urate exporter functioning in both renal and extrarenal urate excretion19506252,20368174,22132962,31003562,36749388. In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates12682043,28554189,30405239. Mediates the secretion of the vitamins riboflavin and biotin into milk (By similarity). Involved in the excretion of the riboflavin-derived compound lumichrome into the intestinal lumen and in its secretion into milk39337371. Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity). Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux11306452,12477054,15670731,18056989,31254042. In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity). In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response

Quoted from UniProt’s FUNCTION annotation for Q9UNQ0 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
ABCC20.9790.1000.8000.889
ABCC10.9710.1000.0000.968
SLCO1B10.8860.0000.0000.886
SLC2A90.8810.0450.0000.873
SLC22A120.8690.0940.0000.860
BSG0.8410.0000.0000.839
MRPS70.8130.0000.0000.813
SLC22A10.8100.0940.0000.798
SLC22A80.8080.0940.0000.796
ALB0.8070.0000.0000.806

Where it sits in the cell

  • Plasma membrane
  • Nucleoplasmadditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cell membrane · Apical cell membrane · Mitochondrion membrane

Expression by cell type

Single cell type RNA, the 6 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Breast lactating cells316.5 nCPM
  • Hofbauer cells298.9 nCPM
  • Enterocytes267.3 nCPM
  • Vascular endothelial cells142 nCPM
  • Extravillous trophoblasts116.4 nCPM
  • Colonocytes104.6 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • intestine83.2 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 1

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Broad substrate specificity ATP-binding cassette transporter ABCG2Drug transportersIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4478426

Other measurements 4

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Broad substrate specificity ATP-binding cassette transporter ABCG2Drug transportersGI50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4478434
Broad substrate specificity ATP-binding cassette transporter ABCG2Drug transportersGI50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4478435
Broad substrate specificity ATP-binding cassette transporter ABCG2Drug transportersGI50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4478436
Broad substrate specificity ATP-binding cassette transporter ABCG2Drug transportersInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4478441