title: Modulation of Expression and Activity of ABC Transporters by the Phytoestrogen Genistein. Impact on Drug Disposition.
abstract: ATP binding cassette (ABC) transporters are involved in drug absorption, distribution and elimination. They also mediate multidrug resistance in cancer cells. Isoflavones, such as genistein (GNT), belong to a class of naturally-occurring compounds found at high concentrations in commonly consumed soya based-foods and dietary supplements. GNT and its metabolites interact with ABC transporters as substrates, inhibitors and/or modulators of their expression. This review compiles information about regulation of ABC transporters by GNT with special emphasis on the three major groups of ABC transporters involved in excretion of endo- and xenobiotics as follows: Pglycoprotein (MDR1, ABCB1), a group of multidrug resistance associated proteins (MRPs, ABCC subfamily) and ABCG2 (BCRP), an ABC half-transporter. The impact of these regulations on potential GNT-drug interactions is further considered.
authors.forename: Juan Pablo
authors.initials: JP
authors.lastname: Rigalli
authors.forename: Nadia
authors.initials: N
authors.lastname: Ciriaci
authors.forename: Aldo Domingo
authors.initials: AD
authors.lastname: Mottino
authors.forename: Viviana Alicia
authors.initials: VA
authors.lastname: Catania
authors.affiliation: Institute of Experimental Physiology, Faculty of Biochemical and Pharmaceutical Science, Rosario National University, Suipacha 570, 2000 Rosario, Argentina. ruiz@ifise-conicet.gov.ar.
authors.forename: María Laura
authors.initials: ML
authors.lastname: Ruiz
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000378:metabolism*; D004347:Drug Interactions; D018432:Drug Resistance, Multiple / Q000187:drug effects; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D019833:Genistein / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D048789:Phytoestrogens / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D018528:ATP-Binding Cassette Transporters; D048789:Phytoestrogens; D019833:Genistein