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Related Concept Videos

Drug Metabolism: Phase I Reactions01:17

Drug Metabolism: Phase I Reactions

A phase I reaction is a biochemical process that introduces a functionally reactive polar group to a substance. This transformation predominantly occurs in the liver, facilitated by the cytochrome P450 system of hemoproteins situated in the lipophilic endoplasmic reticulum of cells. The metabolite generated through this process can have varying polarities. If it is sufficiently polar, it can be easily excreted in the urine due to its water compatibility. However, if the metabolite is nonpolar,...
Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu01:29

Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu

Genetic variations significantly influence drug response through pharmacokinetics, receptor interactions, and biologic milieu modifications. Pharmacokinetic alterations impact drug metabolism and clearance, affecting efficacy and toxicity. Variants in drug-metabolizing enzymes, such as CYP2C9 and CYP2C19, alter drug activation and elimination. For example, CYP2C9 loss-of-function variants require lower warfarin doses to prevent excessive bleeding, while CYP2C19 variants reduce clopidogrel...
Pharmacogenetics of Drug Metabolism: Overview01:27

Pharmacogenetics of Drug Metabolism: Overview

Genetic polymorphism in drug metabolism is crucial to the inter-individual variability observed in drug responses. Drug metabolism primarily involves the chemical modification of drugs and other xenobiotics to enhance their elimination by increasing their polarity. Two main classes of enzymes mediate this biotransformation process: Phase I enzymes, primarily cytochrome P450s, catalyze oxidation and reduction reactions, while other enzymes, such as esterases, mediate hydrolysis, and Phase II...
Pharmacogenetics of Phase I Enzymes: Cytochrome P450 Isozymes01:28

Pharmacogenetics of Phase I Enzymes: Cytochrome P450 Isozymes

Cytochrome P450 (CYP450) enzymes are a superfamily of heme-containing monooxygenases that play a pivotal role in Phase I drug metabolism by catalyzing oxidation and reduction reactions.These enzymes transform lipophilic xenobiotics into more hydrophilic metabolites, facilitating subsequent Phase II conjugation and eventual excretion. The CYP450 family is classified into families (e.g., CYP1–CYP3) and subfamilies (e.g., CYP2A, CYP2C), based on amino acid sequence homology.CYP450 isoenzymes,...
Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase01:27

Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase

Phase II biotransformation reactions are essential for detoxifying and eliminating xenobiotics, including many pharmaceutical compounds. These reactions typically involve conjugation, the covalent attachment of polar endogenous groups such as glucuronic acid, sulfate, methyl, or acetyl moieties to functional groups introduced during Phase I metabolism. The resulting conjugates are more water-soluble, enabling efficient renal or biliary excretion.The major classes of Phase II enzymes include...
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters01:16

Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters

The pharmacogenetics of drug transporters is increasingly recognized as a critical factor influencing interindividual variability in drug absorption, distribution, and elimination. These membrane-bound proteins regulate drugs' movement across cellular barriers by actively pumping them out (efflux) or facilitating their uptake (influx). Among the major transporter families, ATP-binding cassette (ABC) and solute carrier (SLC) transporters play particularly prominent roles. Genetic polymorphisms...

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Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
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Minipig cytochrome P450 3A, 2A and 2C enzymes have similar properties to human analogs.

P Soucek1, R Zuber, E Anzenbacherová

  • 1Group of Biotransformations, Center for Occupational Diseases, National Institute of Public Health, Srobarova 48, Praha 10, 100 42, Czech Republic. psoucek@szu.cz

BMC Pharmacology
|December 12, 2001
PubMed
Summary
This summary is machine-generated.

Minipig liver cytochromes P450 (CYPs) show high N-terminal sequence similarity to human orthologs, supporting their use as models for drug metabolism studies. This research validates minipigs for pharmacological and toxicological research involving human CYP enzymes.

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Area of Science:

  • Pharmacology and Toxicology
  • Biochemistry
  • Comparative Genomics

Background:

  • Minipigs are increasingly considered as experimental models in pharmacology.
  • Their drug-metabolizing systems show similarities to humans.
  • This study focuses on characterizing minipig liver microsomal cytochromes P450 (CYPs).

Purpose of the Study:

  • To characterize minipig liver microsomal cytochromes P450 (CYPs).
  • To compare the N-terminal amino acid sequences of minipig CYPs with their human orthologs.
  • To evaluate the potential of minipigs as models for human drug metabolism.

Main Methods:

  • Partial purification of specific minipig CYP enzymes (2A, 2C, 3A).
  • Identification of purified proteins using antibodies against human CYPs.
  • N-terminal amino acid sequencing and sequence comparison with human CYP orthologs.

Main Results:

  • Minipig CYP2A N-terminal sequence shows 70% identity to human CYP2A6.
  • Minipig CYP2C N-terminal sequence shares approximately 50% similarity with human CYP2C9.
  • Minipig CYP3A N-terminal sequences exhibit 60% identity to human CYP3A4, aligning with pig CYP3A29.

Conclusions:

  • Minipigs possess liver CYP enzymes with high N-terminal sequence similarity to human orthologs.
  • These findings support the use of minipigs as valuable animal models for pharmacological and toxicological studies.
  • Minipigs are particularly suitable for studies involving substrates of human CYP3A and CYP2A enzymes.