Drug Metabolism in Drug Design and Development Basic Concepts and Practice
3.1.6.2 Incubations with Cloned, Expressed Enzymes Individual UGT enzymes have been expressed in a wide variety of systems inclu ...
radiometric HPLC detector or fraction collection and liquid scintillation counting can be employed. The latter method is more se ...
trifluoperazine, hecogenin, and tamoxifen N-glucuronidation appear to be selective for 1A4. Trifluoperazine may be somewhat prob ...
3.1.8.1 Common Drug Metabolizing Enzyme Lamotrigine (LTG) is a diaminotriazine antiepileptic drug that is widely used and promot ...
3.1.8.3 Inhibition of Glucuronide Renal Clearance Glucuronides are cleared by either biliary or renal clearance. Biliary secreti ...
isolation of the phenol sulfate conjugate from human urine. Several years later, the cosubstrate 3^0 -phosphoadenosine 5^0 - pho ...
Sulfonation is generally a detoxification pathway whereby the conjugated product has greater water solubility and is therefore e ...
45% amino acid sequence identity, while subfamily members share at least 60% homology. Each family is designated by an Arabic nu ...
TABLE 3.5 Human SULT isoforms, substrates, and genetic polymorphisms. Human SULT cDNA Substrates Common genetic polymorphisms SU ...
1999; Nagar et al., 2006). Genetic polymorphisms have been reported in SULT1A1, SULT1A2, SULT2A1, SULT1C2, andSULT1E1genes (Tabl ...
achieved on a C18 5U 150 mm 4.6 mm column, with a gradient run of the mobile phase at 20–80% acetonitrile and water containing 0 ...
duodenum (Vietri et al., 2000). The dietary flavonoid quercetin inhibits metabolism of dopamine, minoxidil, salbutamol, acetamin ...
TABLE 3.6 Examples of LC/MS assays employed to study sulfonate conjugates.Substrate LC/MS assay details Ion References Curcumino ...
(Metabolite quantitation) System: LC–MS on a Shimadzu LCMSQP2010A LC: L-column ODs semi-micro; 10 mM ammonium formate pH 3.5 wit ...
3.2.8 Summary Sulfotransferases are important Phase II enzymes that catalyze the conjugation of numerous endogenous chemicals as ...
mitochondria (Pemble et al., 1996). GST classes are abbreviated in Roman capitals and individual members are designated with a n ...
TABLE 3.7 GST nomenclature and tissue expression (Mannervik et al., 2005).Enzymesubunit Class Trivialnames Tissue expression Com ...
species (hydrogen peroxide, OH radicals). There is an antioxidant response element (ARE) in theGSTA1,GSTA3,GSTM1, andGSTP1promot ...
acid changes T122S (conservative) and E210A (at start of external helix). Neither residue was in the active site. When expressed ...
and seven sequence changes in the promoter region. No relationship between any of the identified SNPs was observed in the liver ...
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