Current Drug Metabolism - Volume 10, Issue 7, 2009

This is the second issue of ‘Current Drug Metabolism’ reporting on a variety of areas of drug metabolism contributed by the Editorial Board Members of the journal. The journal, publishing its tenth volume, has received impact factor 4.35 in 2009!! Another milestone development is the launch of a new online manuscript submission and processing system, Contents Management System (CMS; http://bentham-editorial.org Read More

With the advances in recombinant DNA biotechnology, molecular biology and immunology, the number of biotech drugs, including peptides, proteins and monoclonal antibodies, available for clinical use has dramatically increased in recent years. Although pharmacokinetic principles are equally applicable to the large molecule biotech drugs and conventional small molecule drugs, the underlying mechanisms for the proce Read More

The term fatty liver identifies a liver in which lipids account for more than 5% of the liver's wet weight. When fat accumulates, the lipids primarily stored as triglycerides (TG) result in steatosis and provide substrates for lipid peroxidation. Accumulation of neutral lipids in hepatocytes leads to micro- and macro-vesicular steatosis and to balloon-cell degeneration. Increased fat deposition in the liver is generally believed to be th Read More

Cytochrome P450s (P450 or CYPs) comprise a superfamily of enzymes that catalyze the oxidation of a wide variety of xenobiotic chemicals including drugs and environmental carcinogens. Recent studies have demonstrated that endogenous chemicals are also oxidized by human P450s which mainly metabolize xenobiotics. In this review, we summarize the expected physiological significance of the biotransfornation as w Read More

CYP1A2 is one of the major CYPs in human liver (∼13%) and metabolises a variety of clinically important drugs, such as clozapine, lidocaine, theophylline, tacrine, and leflunomide. CYP1A2 is one of the major enzymes that bioactivate a number of procarcinogens and thus induction of CYP1A2 may increase the carcinogenicity of these compounds. This enzyme also metabolizes several important endogenous compound Read More

CYP2B6 is mainly expressed in the liver that has been thought historically to play an insignificant role in human drug metabolism. However, increased interest in this enzyme has been stimulated by the discovery of polymorphic and ethnic differences in CYP2B6 expression, identification of additional substrates for CYP2B6, and evidence for co-regulation with CYP3A4. This paper updates our knowledge about the structure Read More

The CYP2A6 gene spans a region of approximately 6 kb pairs consisting of 9 exons and has been mapped to the long arm of chromosome 19 (between 19q12 and 19q13.2). The CYP2A6 protein has 494 amino acids and is an important hepatic Phase I enzyme that metabolizes ∼3% of therapeutic drugs (n > 30; e.g. valproic acid, pilocarpine, tegafur, fadrozole, ifosfamide, cyclophosphamide, nicotine, tamoxifen, promaz Read More

Human cytochrome P450 2C9 (CYP2C9) accounts for ∼20% of total hepatic CYP content and metabolizes ∼15% clinically used drugs including S-warfarin, tolbutamide, phenytoin, losartan, diclofenac, and celecoxib. To date, there are at least 33 variants of CYP2C9 (*1B through to *34) being identified. CYP2C9*2 and CYP2C9*3 differ from the wild-type CYP2C9*1 by a single point mutation: CYP2C9*2 is characterised by a 430C Read More