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Regulation of Drug Metabolism and Transporters

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Drug metabolizing enzymes (DME) play a central role in the intestinal absorption/permeability, metabolism, elimination and detoxification of endogenous and exogenous compounds. DME include phase I and II metabolizing enzymes. The hydroxylation activity of phase I DME increases the hydrophilicity of the molecules. The electrophilicity of phase I DME-derived products is reduced via conjugation with endogenous ligands, such as glutathione and glucuronic acid, and facilitates their inactivation and excretion in the bile and/or the urine. The transport system is involved in the cellular input/output of molecules and drugs. Numerous endogenous and exogenous compounds, being the substrates of DME, regulate the expression of DME genes through the activation of a number of nuclear receptors. These nuclear receptors directly or indirectly target different regulatory sequences present in the promoter region of the DME genes. The review describes the activation process of nuclear receptors, as well as their interactions to elucidate the extended cross-talk between them in the regulation of DME.

Keywords: Drug metabolizing enzymes; conjugating enzymes; cytochrome P450; gene regulation; nuclear receptors; orphan nuclear receptors; transporters

Document Type: Research Article


Publication date: 2009-10-01

More about this publication?
  • Current Drug Metabolism aims to cover all the latest and outstanding developments in drug metabolism and disposition. The journal serves as an international forum for the publication of timely reviews in drug metabolism. Current Drug Metabolism is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the latest and most important developments. The journal covers the following areas:

    In vitro systems including CYP-450; enzyme induction and inhibition; drug-drug interactions and enzyme kinetics; pharmacokinetics, toxicokinetics, species scaling and extrapolations; P-glycoprotein and transport carriers; target organ toxicity and interindividual variability; drug metabolism and disposition studies; extrahepatic metabolism; phase I and phase II metabolism; recent developments for the identification of drug metabolites and adducts.
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