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ATP-binding cassette sub-family C member 10 (ABCC10) and ATP-binding cassette sub-family G member 2 (ABCG2) (ABCC10; ABCG2)

Target
ABCC10; ABCG2
Molecular classification
Transporter, ATP-binding cassette (ABC) transporter
01

Overview

ATP-binding cassette sub-family C member 10 (ABCC10, also known as MRP7) and ATP-binding cassette sub-family G member 2 (ABCG2, also known as BCRP) are transmembrane proteins that function as ATP-dependent efflux pumps [3, 7]. These transporters are key mediators of multidrug resistance (MDR) in cancer, as they actively extrude a broad spectrum of chemotherapeutic agents, including taxanes, vinca alkaloids, anthracyclines, and antimetabolites, from tumor cells [4, 11]. Beyond their role in oncology, they are endogenously expressed in tissues such as the liver, intestine, and blood-tissue barriers (e.g., blood-brain barrier and placenta), where they protect the body by limiting the absorption and accumulation of xenobiotics [1, 12]. ABCG2 is also uniquely involved in the transport of physiological substrates like uric acid, and its genetic variants are linked to gout and hyperuricemia [7, 15]. ABCC10 transports leukotrienes and steroid conjugates and has been implicated in metabolic and renal health [3, 10]. Therapeutic targeting of these transporters primarily focuses on the use of inhibitors to restore the sensitivity of resistant cancers to chemotherapy, though such interventions must manage the risk of increased systemic toxicity and altered disposition of endogenous compounds [11, 12].

Other names
Multidrug resistance-associated protein 7MRP7Breast cancer resistance proteinBCRPMitoxantrone resistance proteinMXRPlacenta-specific ABC transporterABCPCDw338
02

Mechanism of action

Inhibition of ATP-dependent efflux; Competitive inhibition of substrate transport; Reversal of multidrug resistance

03

Biological functions

ATP-dependent drug effluxXenobiotic transportUrate transportHeme and porphyrin transportLeukotriene C4 transportSteroid hormone conjugate transport
04

Disease associations

Cancer (Multidrug resistance)GoutHyperuricemiaRenal tubular dysfunctionObesity
05

Safety considerations

Increased systemic toxicity of co-administered chemotherapeutic agentsDisruption of blood-brain barrier integrityDisruption of placental barrier protectionPotential for hyperuricemia due to ABCG2 inhibitionAltered pharmacokinetics of endogenous substrates
06

Interacting drugs

Nilotinib

28 more in the full profile.

07

Biomarkers

ABCC10 mRNA/protein expression levelsABCG2 mRNA/protein expression levelsABCG2 c.421C>A (Q141K) polymorphism

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