Target intelligence / Profile preview

Phase II drug-metabolising enzyme (null)

Target
null
Molecular classification
Enzyme, Transferase, Conjugation enzyme
01

Overview

Phase II drug-metabolising enzymes are principally *transferases* that catalyze conjugation reactions—such as glucuronidation, sulfation, acetylation, glutathione conjugation, and methylation—of both endogenous substrates and xenobiotics. The resulting conjugated products are typically less active and more hydrophilic, aiding rapid elimination via urine or feces. Critical Phase II enzymes include UDP-glucuronosyltransferases, sulfotransferases, N-acetyltransferases, glutathione S-transferases, and several methyltransferases. Genetic polymorphisms in these enzymes contribute to interindividual and interspecies differences in drug response and toxicity. These enzymes are central to pharmacogenomics, and alterations in their activity can be linked to cancer risk and adverse drug reactions

Other names
Phase II biotransformation enzymeconjugating enzymedrug-metabolising transferase
02

Mechanism of action

Drugs may act as substrates, inhibitors, or inducers of Phase II enzymes, modifying drug clearance, toxicity, and efficacy

03

Biological functions

Metabolic detoxificationBiotransformation of xenobioticsDrug metabolismInactivation of pharmacologically active compoundsEnhancement of drug excretion
04

Disease associations

Cancer (polymorphisms can affect susceptibility and drug response)Drug toxicity/Adverse drug reactionsPharmacogenomics—variation affects drug efficacy and safety
05

Safety considerations

Drug-drug interactions due to inhibition/inductionGenetic polymorphism leading to variable drug efficacy or toxicityAccumulation of active/toxic metabolites in impaired conjugationIdiosyncratic drug reactions, especially with compromised enzyme activity
06

Interacting drugs

Many clinically used drugs are substrates, including acetaminophen, morphine, codeine, isoniazid, various chemotherapeutics, and others
07

Biomarkers

Genetic polymorphisms (e.g., NAT2 acetylator status, TPMT activity, UGT variants)Enzyme activity levels in tissue or serum

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