Drug Metabolism Enzymes

Drug metabolism enzymes are proteins that chemically modify medicines and other foreign compounds, helping determine how long drugs remain active and how safely they are eliminated. In the liver and other tissues, phase I enzymes, including cytochrome P450 proteins, introduce or expose functional groups through oxidation, reduction, or hydrolysis, while phase II enzymes attach polar molecules such as glucuronic acid or sulfate to improve solubility and excretion. In clinical practice, enzyme activity influences drug dosing, treatment response, adverse effects, and drug interactions because genetic variation, disease, diet, and coadministered medicines can alter metabolic rates. Understanding these pathways supports pharmacokinetic studies, safer prescribing, and individualized therapy.

Drug Metabolism Enzymes - Related Videos

Research

JoVE Journal - Cancer Research

Advancements in the Metabolic Profiling of Three-Dimensional Brain Tumor Spheroids for Drug Screening

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Cited by 1 •

2025

Here, we establish a metabolic profiling platform integrating three-dimensional (3D) glioma spheroids and imaging-based normalization via extracellular flux analysis. This approach enables more accurate assessment of tumor metabolic responses to drug treatments and provides insights into potential mechanisms of resistance.

Education

JoVE Core - Pharmacology

Drug Metabolism: Phase I Reactions

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2023

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,...

Drug Metabolism: Phase II Reactions

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2023

Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...

Pharmacogenetics of Drug Metabolism: Overview

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2026

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...

Methyl Thiazolyl Tetrazolium or MTT Assay: A Colorimetric Assay to Measure Drug Resistance via Determination of Metabolic Activity in Cancer Cells

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2023

This video describes the colorimetric assay, methyl thiazole tetrazolium (MTT) assay, to measure drug-induced cytotoxicity in cancer cells and determine their metabolic activity. This assay is based on the metabolic conversion of tetrazolium salts into colored products, reflecting the mitochondrial activity of cells.

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