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Target intelligence / Profile preview
ATP Binding Cassette Transporter Subfamily G Member 2 (ABCG2)
- Target
- ABCG2
- Molecular classification
- ATP-binding cassette (ABC) transporter, Transporter, Membrane protein, Half-transporter
01
Overview
ABCG2 is an efflux transporter that actively pumps a wide variety of substrates across cellular membranes using energy from ATP hydrolysis. It plays a significant role in multidrug resistance in cancer cells, protects tissues from xenobiotics, regulates drug bioavailability, excretes urate, secretes vitamins, and carries the Jr(a) antigen. Targeted therapeutics are under development to inhibit ABCG2 function for overcoming drug resistance in oncology settings.
- Other names
- BCRPCDw338CD338ABCPMXRMitoxantrone Resistance-associated ProteinJunior blood group antigen carrier
02
Mechanism of action
Efflux of substrates from cells via ATP hydrolysis; inhibition of ABCG2 function to overcome drug resistance
03
Biological functions
Efflux transportMultidrug resistanceXenobiotic detoxificationUrate excretionVitamin secretionBlood group antigen transport
04
Disease associations
Multidrug resistance in cancerCancerPharmacogenomicsTransfusion medicine
05
Safety considerations
Altered drug bioavailabilityDrug-drug interactionsCompromised tissue protection from toxinsReversal of drug resistance may affect normal cell function
06
Interacting drugs
Mitoxantrone
1 more in the full profile.
07
Biomarkers
ABCG2 expression levels in tumor cellsGenetic variants of ABCG2 influencing drug response
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