Drug Metabolism in Drug Design and Development Basic Concepts and Practice
3.3.7.2 Substrates GSTM1-1Trans-stilbene oxide,DCNB-high, CDNB-mod- erate, Aflatoxin B1-exo8,9-epoxide, androstene 3,17-dione, ...
CI = 2.99–4.41) (Schnakenberg E, 2000). Approximately 5–10% of chemical workers exposed to diisocyanates develop asthma and the ...
GSTP1 variants have been identified: P1^ A (104I, 113A), P1^ B (104V, 113A), P1^ C (104V, 113V), and P1^ D (104I, 113V) (Table 3 ...
3.3.9 GST Theta Class 3.3.9.1 Substrates GSTT1-1Dichloromethane, ethylene dibromide, buta- diene diepoxide, cumene hydroperoxi ...
GSTs in liver (GSTA, GSTM, GSTP) can be prepared by affinity chromatography on S-linked glutathione agarose (Sigma G4510) or imm ...
3.3.12 Glutathione Conjugate Metabolism (Mercapturic Acid Pathway) GSH conjugates are highly polar, charged conjugates that cann ...
References Aksoy IA, Weinshilboum RM. Human thermolabile phenol sulfotransferase gene (STM): molecular cloning and structural ch ...
Bossuyt X, Blanckaert N. Functional characterization of carrier-mediated transport of uridine diphosphate N-acetylgylucosamine a ...
Her C, Raftogianis R. et al. Human phenol sulfotransferase STP2 gene: molecular cloning, structural characterization, and chromo ...
Ogilvie BW, Zhang D. et al. Glucuronidation converts gemfibrozil to a potent, metabolism-dependent inhibitor of CYP2C8: implicat ...
Sonoda J, Xie W. et al. Regulation of a xenobiotic sulfonation cascade by nuclear pregnane X receptor (PXR). Proc Natl Acad Sci ...
4 Enzyme Kinetics TIMOTHYS. TRACY 4.1 INTRODUCTION Determination of enzyme kinetic parameters for the metabolism of a new chemic ...
4.2 Enzyme Catalysis The catalysis by enzymes involved in oxidative drug metabolism reactions (e.g., the cytochromes P450) typic ...
4.3.1 Meanings ofKm,Vmaxand Their Clinical Relevance The kinetic parametersKmandVmaxare estimated from the Michaelis–Menten equa ...
than theKm. In this case, the [S] term drops out of the denominator of Eq. 4.1 and the equation reduces to n Vm½S Km ð 4 : 2 Þ ...
very small values ofn, even small errors lead to very large errors in 1/n; this is not noticeable at large values ofn(Dowd and R ...
plot suffers less from the error issues discussed above regarding the double- reciprocal plot and thus, may be the most preferre ...
term allosterism is also used frequently in the P450 literature to refer to the ability of a ligand (a.k.a. effector molecule ot ...
binds to equivalent sites on each protein subunit. However, the advent of more sensitive analytical techniques allowing both acc ...
4.5.2.2 Biphasic Kinetics (Nonasymptotic) For the purposes of this discus- sion, a biphasic kinetic profile is defined as one in ...
«
1
2
3
4
5
6
7
8
9
10
»
Free download pdf