Target intelligence / Profile preview

ATP-binding cassette subfamily C member 1 (ABCC1) (ABCC1)

Target
ABCC1
Molecular classification
Transporter, ATP-binding cassette transporter, Efflux pump
01

Overview

ATP-binding cassette subfamily C member 1 (ABCC1), also known as Multidrug Resistance-associated Protein 1 (MRP1), is a 190 kDa transmembrane protein that functions as an ATP-dependent efflux pump [1, 8]. It mediates the transport of a wide variety of substrates, including hydrophobic drugs and organic anions conjugated with glutathione, glucuronide, or sulfate [1, 2]. Originally identified for its role in conferring multidrug resistance in cancer cells by extruding chemotherapeutic agents such as anthracyclines and vinca alkaloids, it is now recognized for its essential physiological roles [3, 6]. ABCC1 is ubiquitously expressed in normal tissues, where it is primarily localized to the basolateral membrane and serves to maintain protective barriers, such as the blood-brain and blood-testis barriers [4, 11]. It also plays a critical role in inflammatory responses by transporting the pro-inflammatory mediator leukotriene C4 and participates in cellular redox homeostasis through the transport of glutathione [1, 9]. In clinical oncology, ABCC1 expression levels and genetic variants are used as biomarkers to predict chemotherapy response and potential toxicity [12, 13].

Other names
Multidrug resistance-associated protein 1MRP1LTC4 transporterGlutathione-S-conjugate-translocating ATPase ABCC1ABC29GS-X pump
02

Mechanism of action

ATP-dependent active efflux of substrates, competitive and non-competitive inhibition of transporter activity, and chemosensitization of multidrug-resistant cells [1, 5].

03

Biological functions

ATP-dependent active effluxXenobiotic transportLeukotriene C4 transportGlutathione conjugate transportRedox homeostasisCellular detoxificationTissue barrier maintenance
04

Disease associations

CancerMultidrug resistanceInflammationNeurodegenerative diseaseCardiovascular disease
05

Safety considerations

Increased systemic toxicity of chemotherapeutic substratesDisruption of physiological leukotriene signalingImpairment of tissue-barrier protection (e.g., blood-brain barrier)Pharmacokinetic drug-drug interactions (DDIs)
06

Interacting drugs

Vincristine

9 more in the full profile.

07

Biomarkers

ABCC1 mRNA expression levelsABCC1 protein expressionABCC1 germline single nucleotide polymorphisms (SNPs)

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