Structure, function, expression, genomic organization, and single nucleotide polymorphisms of human ABCB1 (MDR1), ABCC (MRP), and ABCG2 (BCRP) efflux transporters.

摘要: The ATP-binding cassette (ABC) transporters constitute a large family of membrane proteins, which transport variety compounds through the against concentration gradient at cost ATP hydrolysis. Substrates ABC include lipids, bile acids, xenobiotics, and peptides for antigen presentation. As they exogenous endogenous compounds, reduce body load potentially harmful substances. One by-product such protective function is that also eliminate various useful drugs from body, causing drug resistance. This review brief summary structure, function, expression important resistance-conferring members belonging to three subfamilies human family; these are ABCB1 (MDR1/P-glycoprotein subfamily ABCB), ABCC (MRPs), ABCG2 (BCRP ABCG), expressed in organs. In text, transporter symbol carries name (such as ABCB1, ABCC1, etc.) used interchangeably with corresponding original names, MDR1P-glycoprotein, MRP1, etc., respectively. Both nomenclatures maintained text because both still literature. helps readers relate names encounter It now appears P-glycoprotein, MRP2, BCRP can explain phenomenon multidrug resistance all cell lines analyzed thus far. Also discussed gene regulation expression, polymorphisms genes. Because genetic polymorphism thought underlie interindividual differences, including their response other importance genes discussed.