title: ABC drug transporters as molecular targets for the prevention of multidrug resistance and drug-drug interactions.
abstract: ABC transporters play an important role in mediating the cytoplasmic concentration of endogenous and xenobiotic substances. They therefore influence the pharmacokinetic profile of a variety of drugs. By virtue of their localization to plasma membranes in the intestine, liver, blood-brain and other vital biological barriers, a majority of ABC drug transporters cause drug-drug interactions, decreased drug efficacy and multidrug resistance for chemotherapeutic agents. Thus, elucidating which drug entities are substrates for ABC drug transporters is a crucial step in the drug development and treatment process. Here, we review the current status of methodology used to categorize drug compounds as substrates or modulators for the major ABC drug transporters including ABCB1, ABCC1 and ABCG2.
authors.affiliation: Laboratory of Cell Biology, Center for Cancer Research, National Cancer Institute, NIH/DHHS, Bethesda, MD 20892, USA. calcagnoa@mail.nih.gov
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Calcagno
authors.forename: In-Wha
authors.initials: IW
authors.lastname: Kim
authors.forename: Chung-Pu
authors.initials: CP
authors.lastname: Wu
authors.forename: Suneet
authors.initials: S
authors.lastname: Shukla
authors.forename: Suresh V
authors.initials: SV
authors.lastname: Ambudkar
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000187:drug effects* / Q000378:metabolism; D000818:Animals; D001692:Biological Transport; D016503:Drug Delivery Systems; D015195:Drug Design; D004347:Drug Interactions; D018432:Drug Resistance, Multiple; D006801:Humans; D010599:Pharmacokinetics
chemical_list: D018528:ATP-Binding Cassette Transporters