Download Cytochrome P450 2D6: Structure, Function, Regulation and by Shufeng Zhou PDF

By Shufeng Zhou

Cytochromes are proteins that catalyze electron move reactions of famous metabolic pathways and are categorised in a variety of superfamilies. The CYP, or P450, superfamily bills for ninety% of the oxidative metabolism of medical medications. One member of this superfamily, P450 2D6 (or CYP2D6), singlehandedly metabolizes approximately 25% of all medicines within the human liver. Cytochrome P450 2D6: constitution, functionality, rules, and Polymorphism studies the present wisdom of CYP2D6 in addition to the maturing physique of proof indicating its importance to medical and pharmacological researchers and practitioners.

This ebook specializes in the severe position CYP2D6 performs within the human liver. It examines the genetic, epigenetic, physiological, pathological, and structural components of the gene that govern the hugely variable metabolism of a couple of medicines in scientific use. It highlights the influence of the sensible roles of CYP2D6 on medical perform and drug improvement and likewise discusses implications for exact drugs, recommendations to prevent adversarial drug reactions, and paths for destiny research.

Cytochrome P450 2D6

is a special, invaluable booklet concentrating on a unmarried yet immensely strong human gene. It offers the 1st unmarried resource of entire details on CYP2D6 that serves as a massive reference for scientific, biomedical, pharmaceutical, and nursing researchers, practitioners, and students.

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Cytochrome P450 2D6: Structure, Function, Regulation and Polymorphism

Cytochromes are proteins that catalyze electron move reactions of recognized metabolic pathways and are categorized in numerous superfamilies. The CYP, or P450, superfamily debts for ninety% of the oxidative metabolism of medical medications. One member of this superfamily, P450 2D6 (or CYP2D6), singlehandedly metabolizes approximately 25% of all medicines within the human liver.

Additional resources for Cytochrome P450 2D6: Structure, Function, Regulation and Polymorphism

Example text

1C is reported to cause decreased inducibility of the enzyme in Japanese smokers, probably owing to decreased enzyme expression (Nakajima et al. 1999). , smoking) (Sachse et al. 1999), although this association is controversial (Aklillu et al. 2003; Chida et al. 1999; Larsen and Brosen 2005; Nordmark et al. 2002; Shimoda et al. 2002). Smokers with the −163C/C genotype have 40% lower plasma 17X/137X ratios compared with those with the −163A/A genotype in smokers (Sachse et al. 1999). *1J (−163C>A; −7391T>G) and *1K (−163C>A; −739T>G; −729C>T) have been detected in Ethiopians (Aklillu et al.

IL-6 treatment significantly induces CYP1B1 and 2E1, but not 1A1, in colorectal cancer HCT116 and SW480 cells (Patel et al. 2014). The regulation of CYP2E1 expression by IL-6 is via a transcriptional mechanism involving signal transducer and activator of transcription 3 (STAT3)–mediated pathway while IL-6 downregulates the CYP1B1-targeting miR27b through modulation of DNA methylation (Patel et al. 2014). A study in healthy volunteers has shown that inflammatory response to even a very low dose of lipopolysaccharide significantly decreases CYP1A2 and 2C19 activities (Shedlofsky et al.

CYP1A1 and 1A2 are also involved in the bioactivation and detoxification of the herbal nephrotoxic and carcinogenic compound aristolochic acid (Levova et al. 2011; Sistkova et al. 2008; Stiborova et al. 2012). CYP1A1 can metabolize endogenous substrates including the endogenous fatty acid precursors of PGs such as AA and eicosapentaenoic acid (EPA) (Arnold et al. 2010; Schwarz et al. J. Lee et al. 2003), and melatonin (X. Ma et al. 2005; Yeleswaram et al. 1999). CYP1A1 together with 1A2, 1B1, and 3A4 catalyze the 2-, 4-, and 16α-hydroxylation of 17β-estradiol (Badawi et al.

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