Drug Metabolism in Drug Design and Development Basic Concepts and Practice
2C19 and 2D6 might be expected in the future as development strategies select against these. In the following sections, the abbr ...
xenobiotics, with about five dominant in drug metabolism (Fig. 2.1b). The functions of1/4 of the P450s are still largely unchar ...
de Montellano and De Voss, 2005). Some of these transformations are shown in Fig. 2.4, but the list is certainly not comprehensi ...
although the range of substrates is much more restricted. The substrates are generally soft nucleophiles, almost always N, S, an ...
Mitchell, 1972), and care should be taken so as not to overlook possible contributions of this enzyme. The C-4a-hydroperoxide is ...
2.5.4 Aldehyde Oxidase and Xanthine Dehydrogenase These two enzymes are found in the cytosol of the liver (and other tissues) an ...
Thus, the Mo center is involved in the oxidation of the substrate. In the mechanism, the source of the oxygen atom inserted into ...
for example, X(+H+)!HOX, which can do various types of chemistry and other peroxidases acting on acetaminophen (to generate the ...
functional ALDH genes (Vasiliou and Nebert, 2005). In animal models, some of the ALDHs are inducible by barbiturates or by ligan ...
2.6.2 NADPH-P450 Reductase The normal functions of this flavoprotein are to transfer electrons from NADPH to P450 (and to heme o ...
2.6.3 Aldo-Keto Reductases (AKR) The AKRs constitute a large family of enzymes involved in reduction of various aldehydes and ke ...
Similarly, iminoquinones can be reduced, and the enzymes can also reduce nitro compounds and azo dyes (Ross, 1997). NQO1 was fir ...
2003). P450s convert many olefins and aromatic compounds to epoxides that, unless hydrolyzed or conjugated, can react with tissu ...
drugs, behind P450s and UGTs (Fig. 2.1a). These enzymes are collectively found in many places, including the liver and plasma. O ...
Burka LT, Guengerich FP, Willard RJ, Macdonald TL. Mechanism of cytochrome P-450 catalysis. Mechanism of N-dealkylation and amin ...
Guengerich FP. Biotransformation, Vol. 3, Compr Toxicology, first ed. Elsevier Science, Oxford; 1997. Guengerich FP. Human cytoc ...
Kurosaki M, Terao M, Barzago MM, Bastone A, Bemardinello D, Salmona M, Garattini E. The aldehyde oxidase gene cluster in mice an ...
Rendic S. Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev 2002;34:83–448. Ross D. Quinon ...
...
3 Conjugative Metabolism of Drugs RORYREMMEL,SWATINAGAR ANDUPENDRAARGIKAR 3.1 UDP-Glucuronosyltransferases Glucuronidation is th ...
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