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Related Concept Videos

Phase II Reactions: Glucuronidation01:24

Phase II Reactions: Glucuronidation

Glucuronidation, a pivotal phase II biotransformation process, involves the coupling of glucuronic acid to a drug or xenobiotic. Given its widespread occurrence and critical role in drug metabolism, it's considered the most crucial phase II reaction. It enhances the water solubility of substances, aiding their expulsion from the body. The driving force behind these reactions is a group of enzymes known as UDP-glucuronosyltransferases (UGTs). UGTs facilitate the transfer of a glucuronic acid...
Drug Metabolism: Phase II Reactions01:14

Drug Metabolism: Phase II Reactions

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 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...
Phase II Reactions: Sulfation and Conjugation with α-Amino Acids01:19

Phase II Reactions: Sulfation and Conjugation with α-Amino Acids

Sulfation and α-amino acid conjugation are two critical biotransformation reactions in drug metabolism. Sulfation, a phase II biotransformation reaction, involves adding a polar sulfate group to a drug, enhancing its water solubility and promoting excretion. This process can either co-occur with or occur independently of glucuronidation. Nonmicrosomal sulfotransferase enzymes catalyze the process. The reaction involves 3'-phosphoadenosine-5'-phosphosulfate or PAPS coenzyme activation, sulfur...
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
Drug Biotransformation: Overview01:16

Drug Biotransformation: Overview

Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...

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Related Experiment Video

Updated: May 26, 2026

Regioselective O-Glycosylation of Nucleosides via the Temporary 2',3'-Diol Protection by a Boronic Ester for the Synthesis of Disaccharide Nucleosides
08:46

Regioselective O-Glycosylation of Nucleosides via the Temporary 2',3'-Diol Protection by a Boronic Ester for the Synthesis of Disaccharide Nucleosides

Published on: July 26, 2018

Steroid UDP glucuronosyltransferases.

P I Mackenzie1, L Rodbourne, S Stranks

  • 1Department of Clinical Pharmacology, School of Medicine, Flinders Medical Centre, Bedford Park, SA, Australia.

The Journal of Steroid Biochemistry and Molecular Biology
|January 6, 2012
PubMed
Summary
This summary is machine-generated.

Steroid glucuronidation, essential for elimination, can form reactive compounds. The UGT2B subfamily, particularly UGT2B enzymes, plays a key role in this process, with implications for hormonal balance and disease diagnosis.

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Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
14:57

Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases

Published on: October 10, 2020

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Last Updated: May 26, 2026

Regioselective O-Glycosylation of Nucleosides via the Temporary 2',3'-Diol Protection by a Boronic Ester for the Synthesis of Disaccharide Nucleosides
08:46

Regioselective O-Glycosylation of Nucleosides via the Temporary 2',3'-Diol Protection by a Boronic Ester for the Synthesis of Disaccharide Nucleosides

Published on: July 26, 2018

Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
14:57

Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases

Published on: October 10, 2020

Area of Science:

  • Biochemistry
  • Pharmacology
  • Endocrinology

Background:

  • Steroid glucuronidation is crucial for steroid elimination via bile and urine.
  • Steroid glucuronides are generally less reactive than parent steroids, but toxic forms can arise in disease or therapy.
  • Blood concentrations of steroid glucuronides can signal hormonal imbalances and serve as diagnostic markers for steroid synthesis/metabolism defects.

Purpose of the Study:

  • To review UDP-glucuronosyltransferases (UGTs) involved in steroid glucuronidation.
  • To describe UGT specificities, functional domains, and regulation in steroid metabolism.
  • To highlight the role of the UGT2B subfamily in steroid glucuronidation.

Main Methods:

  • Review of existing literature on steroid glucuronidation and UGT enzymes.
  • Analysis of UGT specificities, domains, and regulatory mechanisms.
  • Examination of evidence from rat studies with implications for human physiology.

Main Results:

  • Steroid glucuronidation is primarily mediated by the UGT2B subfamily.
  • UGT2B enzymes are encoded by 6-exon genes.
  • Regioselectivity in steroid glucuronidation is determined by domains encoded by exons 1 and 2.

Conclusions:

  • The UGT2B subfamily is central to steroid glucuronidation.
  • Specific domains within UGT2B proteins dictate regioselectivity.
  • Findings in rats suggest a similar mechanism in humans, warranting further investigation.