Parasite ATP-binding cassette transporter (ABC transporter) (ABC transporter)

Parasite ATP-binding cassette (ABC) transporters are essential transmembrane proteins that utilize the energy derived from ATP hydrolysis to translocate various substrates across biological membranes [1, 4]. In pathogenic parasites such as Plasmodium falciparum, Leishmania spp., and parasitic helminths, these transporters—particularly P-glycoprotein-like efflux pumps—function as a primary defense mechanism against antiparasitic drugs [1, 3]. By actively pumping out toxic compounds, these proteins reduce the intracellular concentration of essential medications like chloroquine, mefloquine, and ivermectin, leading to the development of multidrug resistance (MDR) [2, 3]. Consequently, these transporters are significant therapeutic targets; inhibiting their activity can chemosensitize parasites and restore the efficacy of existing treatments [1, 5]. However, the high degree of conservation between parasite ABC transporters and human homologs, such as the human multidrug resistance protein 1 (MDR1), necessitates the development of highly selective inhibitors to avoid systemic toxicity and adverse drug-drug interactions in the host [3, 4].

Other names

P-glycoprotein-like efflux pumpMultidrug resistance proteinMDR proteinABC superfamily transporterEfflux pumpParasite P-glycoprotein

Inhibition of ATP-dependent efflux to increase intracellular drug concentration and restore parasite sensitivity to antiparasitic agents [1, 3].