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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Modulation of Expression and Activity of ABC Transporters by the Phytoestrogen Genistein. Impact on Drug Disposition

Author(s): Juan Pablo Rigalli, Nadia Ciriaci, Aldo Domingo Mottino, Viviana Alicia Catania and María Laura Ruiz

Volume 23, Issue 13, 2016

Page: [1370 - 1389] Pages: 20

DOI: 10.2174/0929867323666160406120711

Price: $65


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.

Keywords: ATP binding cassette transporters, breast cancer resistance protein, genistein, multidrug resistanceassociated proteins, nutrient-drug interactions, P-glycoprotein, xenobiotic transport.

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