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Related Concept Videos

Phase II Reactions: Glucuronidation01:24

Phase II Reactions: Glucuronidation

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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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Drug Metabolism: Phase II Reactions01:14

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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...
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Biosynthesis of Polysaccharides01:26

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Polysaccharides such as glycogen and starch are synthesized from nucleoside diphosphate sugars, primarily uridine diphosphate glucose (UDPG) and adenosine diphosphate glucose (ADPG). These activated glucose donors act as key intermediates in carbohydrate metabolism and biosynthesis. UDPG primarily involves glycogen synthesis in animals and many bacteria, while ADPG plays a fundamental role in starch synthesis in plants and certain bacteria.UDPG is formed when glucose-1-phosphate reacts with...
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Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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Related Experiment Video

Updated: Jul 15, 2025

Uracil-DNA Glycosylase Assay by Matrix-assisted Laser Desorption/Ionization Time-of-flight Mass Spectrometry Analysis
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Small Molecules Targeting Human UDP-GlcNAc 2-Epimerase.

Jacob L Gorenflos López1,2, Gillian L Dornan1, Nico Boback3

  • 1Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Robert-Rössle-Strasse 10, 13125, Berlin, Germany.

Chembiochem : a European Journal of Chemical Biology
|September 28, 2023
PubMed
Summary
This summary is machine-generated.

Researchers identified three potent small molecule inhibitors for Uridine diphosphate N-acetylglucosamine 2-epimerase (GNE), a key enzyme in sialic acid biosynthesis. These non-carbohydrate compounds show promise for modulating sialic acid production.

Keywords:
carbohydrate biosynthesishigh-throughput screening campaignoligomerisation inhibitorsreal-time NMRuridine diphosphate N-acetylglucosamine 2-epimerase

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Visualizing Intracellular Sialylation with Click Chemistry and Expansion Microscopy
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Area of Science:

  • Biochemistry
  • Enzymology
  • Glycobiology

Background:

  • Sialic acids are crucial terminal glycans involved in numerous biological processes and diseases.
  • Uridine diphosphate N-acetylglucosamine 2-epimerase (GNE) is a critical enzyme in the sialic acid biosynthesis pathway.
  • Developing non-carbohydrate GNE inhibitors is essential for therapeutic strategies targeting sialic acid metabolism.

Purpose of the Study:

  • To discover and characterize novel, non-carbohydrate small molecule inhibitors of GNE.
  • To evaluate the potency and mechanism of action of identified GNE inhibitors.
  • To assess the potential of these inhibitors for modulating sialic acid biosynthesis.

Main Methods:

  • High-throughput screening of 68,640 drug-like small molecules against recombinant GNE.
  • Validation using real-time NMR assays and manual IC50 determination.
  • Biophysical characterization including thermal shift assays, SEC, and iSCAM.
  • Mechanism of action studies using hydrogen-deuterium exchange mass spectrometry (HDX-MS).

Main Results:

  • Identified nine primary GNE inhibitors from high-throughput screening, with IC50 values in the low micromolar to nanomolar range.
  • Three compounds demonstrated favorable stability and solubility profiles.
  • Inhibitors were shown to affect the oligomeric state of GNE.
  • HDX-MS elucidated the binding regions of GNE targeted by the inhibitors.

Conclusions:

  • Three potent small molecule GNE inhibitors were identified in vitro.
  • These compounds represent promising leads for modulating sialic acid biosynthesis.
  • The identified inhibitors offer a non-carbohydrate scaffold for future drug development.