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Related Concept Videos

Phase II Reactions: Glutathione Conjugation and Mercapturic Acid Formation01:22

Phase II Reactions: Glutathione Conjugation and Mercapturic Acid Formation

Glutathione, a tripeptide made up of glutamate, cysteine, and glycine, is a critical player in the detoxification of drugs and xenobiotics via a process known as glutathione conjugation or mercapturic acid formation. This phase II biotransformation reaction involves the covalent binding of glutathione to a drug or its metabolite, enhancing the compound's water solubility and enabling its excretion.
Several distinctive characteristics distinguish glutathione conjugation from other phase II...
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...
Glucose Transporters01:27

Glucose Transporters

Glucose transporters facilitate the transport of glucose across the cell membrane. In addition to glucose, some glucose transporters can also aid the movement of other hexoses such as fructose, mannose, and galactose.
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:
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...
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...

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Related Experiment Video

Updated: Jun 3, 2026

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

Sigma-class glutathione transferases.

Jack U Flanagan1, Mark L Smythe

  • 1The University of Auckland, Auckland Cancer Society Research Center, Grafton, Auckland, New Zealand. j.flanagan@auckland.ac.nz

Drug Metabolism Reviews
|March 24, 2011
PubMed
Summary
This summary is machine-generated.

Sigma-class glutathione transferases (GSTs) are vital enzymes found across species, performing diverse roles from detoxification to immune modulation. Understanding their structure and function offers therapeutic potential for conditions like allergic responses.

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Rapid Quantification of Oxidized and Reduced Forms of Glutathione Using Ortho -phthalaldehyde in Cultured Mammalian Cells In Vitro
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Rapid Quantification of Oxidized and Reduced Forms of Glutathione Using Ortho -phthalaldehyde in Cultured Mammalian Cells In Vitro

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Last Updated: Jun 3, 2026

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

Rapid Quantification of Oxidized and Reduced Forms of Glutathione Using Ortho -phthalaldehyde in Cultured Mammalian Cells In Vitro
03:35

Rapid Quantification of Oxidized and Reduced Forms of Glutathione Using Ortho -phthalaldehyde in Cultured Mammalian Cells In Vitro

Published on: June 28, 2024

Area of Science:

  • Biochemistry
  • Enzymology
  • Immunology

Background:

  • Mammalian cytosolic glutathione transferases (GSTs) are classified into seven distinct groups.
  • The sigma-class GST is evolutionarily conserved, present in both vertebrates and invertebrates, indicating significant biological importance.
  • Sigma-class GSTs exhibit diverse specialized functions, including roles in vision (cephalopod S-crystallins), prostaglandin metabolism, and parasite antigenicity.

Purpose of the Study:

  • To review the structure, function, and pharmacology of sigma-class GSTs in both vertebrates and invertebrates.
  • To highlight the specialized roles and physiological significance of sigma-class GSTs.
  • To explore the therapeutic potential of targeting sigma-class GSTs, particularly in allergic conditions.

Main Methods:

  • Review of existing literature on sigma-class glutathione transferases.
  • Analysis of studies involving genetic manipulation (depletion and overexpression) of sigma-class GST in mice.
  • Examination of structure-based drug design approaches for sigma-class GST inhibitors.

Main Results:

  • Sigma-class GSTs possess dual roles in mammalian immune responses, acting as both anti- and pro-inflammatory agents.
  • Invertebrate sigma-class GSTs are implicated in detoxification, such as processing lipid oxidation products in flies.
  • Genetic studies in mice reveal critical physiological functions of sigma-class GST.
  • Structure-based inhibitors targeting mammalian sigma-class GST demonstrate efficacy in managing allergic responses.

Conclusions:

  • Sigma-class GSTs are versatile enzymes with critical roles in diverse biological processes across the animal kingdom.
  • Their involvement in immune modulation and detoxification highlights their significance in health and disease.
  • Targeting sigma-class GSTs represents a promising pharmacological strategy for treating inflammatory and allergic diseases.