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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