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Microsoft word - tables greim15-7-2006.doc

Table 1. Phase I and phase II are metabolic processes. Hydrophilic compound do
not need metabolism to be excreted.
Hydrophilic Lipophilic
compound compound
Table 2. Phase I, Phase II and Phase III enzymes
Monoamine oxidases (MAO) Cyclooxygenases (COX) DT-Diaphorases (NQOR) Alcohol dehydrogenases (ADH)
Transferases Glutathiontransferases (GST) Sulfotransferases (SULT) Acetyltransferases (NAT)
Phase III-Enzymes:
Transporters Organic anion-transporting polypeptides (OATP) ATP Binding Cassette transporter family B1 (ABCB1)1 ATP Binding Cassette transporter family C1 (ABCC1)2 2 Multidrug resistance-associated proteins (MRP) Table 3. Changes of lipophilicty of compounds by metabolism. Phase II is more
efficient in changing lipophilicity than phase I.
1octanol/water partition coefficient. Logarithm of partition coefficient, P=[Organic] / [Aqueous]. Octanol models body fat, water models body water Table 4. Human and mouse putuative ful -length CYP genes. Currently 57 Human
CYP genes are known (and 58 pseudogenes). This number is expected to be
complete. Each gene additional y has its al elic variants.
B Subfamilies in mice with only pseudogene orthologs in humans The gene names are listed numerical y and alphabetical y by subfamilies, and pairing does not necessarily denote orthologous genes, e.g. it is not known whether human CYP2A6 is the ortholog of mouse Cyp2a4. Genes having the identical combination of numbers and letters are orthologs between the two species (adapted from Nelson et al. Pharmacogenetics, 2004).
Table 5. In vivo substrates for cytochrome P450 enzymes.
Marker substrate
Marker substrate
Remark: CYP1A1 is only present after induction Table 6. Quantitation of and quantitative role in xenobiotica metabolism of
cytochrome P450 isoenzymes. Amount of cytochrome P450 in liver was determined
by immunoquantitation. Participation of cytochrome P450 enzymes in metabolism of drugs is estimated. CYP2D6 is overrepresented in drug metabolism. Table 7. Functional polymorphisms of cytochrome P450 enzymes
CYP enzyme
Wild-type allele
Most frequent genotype to
yield poor metabolism
Table 8. Polymorphism of cytochromes P450 with clinical relevance and their probe
substrate. Almost al phase I enzymes exhibit genomic polymorphisms. Most phase I
enzymes exhibit clinical y relevant genetic polymorphisms. However, the polymophisms listed below are general y accepted and more frequently encountered.
Cytochrome1 Phenotype
In-vivo probe4
with mutation
ß-blockers, i.e. propafenone Antidepressants, i.e imipramine 1 for more polymorphisms see and eles/, accessed January 2006 3 for more substrates see and, accessed january 2006 Table 9. Subdivision of esterases as subfamilies of α, ß-hydrolases
Abbreviation Substrate


Microsoft word - lope de vega y castro adaptaciÓn total.doc

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