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      Mammalian drug efflux transporters of the ATP binding cassette (ABC) family: an overview

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      Advanced Drug Delivery Reviews

      Elsevier BV

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          Abstract

          Active drug efflux transporters of the ATP binding cassette (ABC)-containing family of proteins have a major impact on the pharmacological behavior of most of the drugs in use today. Pharmacological properties affected by ABC transporters include the oral bioavailability, hepatobiliary, direct intestinal, and urinary excretion of drugs and drug-metabolites and -conjugates. Moreover, the penetration of drugs into a range of important pharmacological sanctuaries, such as brain, testis, and fetus, and the penetration into specific cell- and tissue compartments can be extensively limited by ABC transporters. These interactions with ABC transporters determine to a large extent the clinical usefulness, side effects and toxicity risks of drugs. Many other xenotoxins, (pre-)carcinogens and endogenous compounds are also influenced by the ABC transporters, with corresponding consequences for the well-being of the individual. We aim to provide an overview of properties of the mammalian ABC transporters known to mediate significant transport of clinically relevant drugs.

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          Author and article information

          Journal
          Advanced Drug Delivery Reviews
          Advanced Drug Delivery Reviews
          Elsevier BV
          0169409X
          January 2003
          January 2003
          : 55
          : 1
          : 3-29
          Article
          10.1016/S0169-409X(02)00169-2
          12535572
          5b52b487-6306-4353-81b7-414f82b6ba48
          © 2003

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