Multidrug resistance-associated protein 1 (MRP1) (MRP1)

Multidrug resistance-associated protein 1 (MRP1), encoded by the ABCC1 gene, is a primary member of the ATP-binding cassette (ABC) transporter superfamily (UniProt P33527). It functions as an ATP-dependent efflux pump that transports a broad range of substrates, including anticancer drugs, glutathione-conjugated xenobiotics, and endogenous signaling molecules like leukotriene C4 (Cole, 2014). In the context of oncology, MRP1 is a major driver of multidrug resistance (MDR), as its overexpression allows tumor cells to actively expel chemotherapeutic agents, thereby reducing their intracellular concentration and therapeutic efficacy (Munoz et al., 2007). Beyond its role in cancer, MRP1 is essential for protecting tissues from oxidative stress and regulating inflammatory responses by mediating the export of pro-inflammatory mediators (Robbiani et al., 2000). Therapeutic efforts have focused on developing MRP1 inhibitors to reverse drug resistance, although clinical success has been limited by the need for high selectivity to avoid systemic toxicity (Szakács et al., 2006).

Other names

ABCC1ATP-binding cassette sub-family C member 1Leukotriene C4 export pumpGS-X pumpMRP

ATP-dependent efflux of substrates from the intracellular space to the extracellular environment, often involving co-transport with or conjugation to glutathione.