Target intelligence / Profile preview

ATP-binding cassette transporter G member 2 (ABCG2)

Target
ABCG2
Molecular classification
Transporter, ATP-binding cassette (ABC) transporter, Membrane protein, Multidrug transporter
01

Overview

ATP-binding cassette transporter G member 2 (ABCG2), also known as Breast cancer resistance protein (BCRP), is a membrane-bound half-transporter from the G subfamily of ATP-binding cassette (ABC) transporters[1][2]. This protein functions primarily as an efflux pump, utilizing ATP hydrolysis to export a wide range of substrates, including chemotherapeutic drugs, porphyrins, steroids, and other xenobiotics, out of cells[1][2][5]. ABCG2 is implicated in multidrug resistance in various cancers, affecting the absorption, distribution, and elimination of numerous pharmaceuticals[1][2]. In addition to its role in cancer, ABCG2 participates in physiological processes such as porphyrin homeostasis, and genetic variants have been linked to disorders such as gout[5]. It represents an important therapeutic target for overcoming drug resistance and modulating drug bioavailability.

Other names
Breast cancer resistance proteinBCRPATP-binding cassette sub-family G member 2
02

Mechanism of action

Drug efflux (active transport of drugs out of cells via ATP hydrolysis) Limiting intracellular concentration of chemotherapeutics Modulating absorption and distribution of drugs

03

Biological functions

Multidrug resistanceCellular transport of xenobiotics and endogenous substancesPorphyrin homeostasisSteroid and lipid transport
04

Disease associations

Cancer (notably chemotherapy resistance)Porphyrin metabolism disordersPotentially other disorders involving xenobiotic/drug handling
05

Safety considerations

Chemotherapy failure due to drug resistanceRisk of altered drug pharmacokinetics leading to toxicity or reduced efficacyPossible drug-drug interactions due to broad substrate specificity
06

Interacting drugs

Mitoxantrone

4 more in the full profile.

07

Biomarkers

ABCG2/BCRP expression as a biomarker for multidrug resistance in cancerABCG2 mutations in gout and porphyrin disorders

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