Multidrug resistance proteins: role of P-glycoprotein, MRP1, MRP2, and BCRP (ABCG2) in tissue defense

Transcriptional expression analysis of ABC efflux transporters and xenobiotic-metabolizing enzymes in the Chinese rare minnow

“…In humans, 49 ABC genes organized into seven subfamilies (A-G) have been described (Dean and Annilo, 2005;Lončar et al, 2010). Despite the large number of ABC proteins, previous studies have revealed that the P-glycoprotein (ABCB1), the Bile Salt Export Pump (BSEP; ABCB11), the multidrug resistanceassociated proteins 1-5 (ABCC1-5), and the breast cancer resistance protein (ABCG2) are the most toxicologically relevant proteins in mammals (Leslie et al, 2005;Szakacs et al, 2008). Though there is some overlap in the substrate specificity of these ABC transporters, there are differences in their transport mechanisms (Costa et al, 2012).…”

Molecular analysis, developmental function and heavy metal-induced expression of ABCC5 in zebrafish

“…They are capable of preventing the uptake of toxic compounds, including many drugs and food components, from the gut into the body. MRPs are also essential for protecting vital structures in the body, such as brain, cerebrospinal fluid, testis, and fetus, against toxins that enter the body (Leslie et al, 2005).…”

Determination and modelling of stereoselective interactions of ligands with drug transporters: A key dimension in the understanding of drug disposition

“…Pgp is a member of the ATP-binding cassette (ABC) transporter family that includes the multidrug resistance proteins (MRP1, MRP2) and breast cancer resistance protein (BCRP) (Leslie et al 2005; see also the papers in this issue). The expression and functional activity of these proteins in tumour cell lines has been associated with the reduced sensitivity of these cells to treatment by anticancer agents such as anthracycline antibiotics and vinca alkaloids (cf.…”

“…The expression and functional activity of these proteins in tumour cell lines has been associated with the reduced sensitivity of these cells to treatment by anticancer agents such as anthracycline antibiotics and vinca alkaloids (cf. Spiegl-Kreinecker et al 2002; Leslie et al 2005). Thus, the identification and development of inhibitors of ABC-transporter mediated drug efflux has been an important part of oncology research programs (cf.…”