Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Golgi Matrix Proteins01:12

Golgi Matrix Proteins

2.0K
Golgi matrix proteins are a group of highly dynamic proteins that maintain the stacked structure of Golgi. These proteins adapt to rapid morphological changes of the Golgi during the cell cycle. During cell division, mild proteolysis removes these connections resulting in Golgi unstacking. In The daughter cells, these proteins help reassemble the unstacked Golgi.
One of the first identified Golgi matrix proteins was GM130, a rod-like protein located in the cis-Golgi. Subsequently, many Golgi...
2.0K
Oligosaccharide Assembly01:24

Oligosaccharide Assembly

2.8K
Protein glycosylation starts in the ER lumen and continues in the Golgi apparatus. Glycosyltransferases catalyze the addition of sugar molecules or glycosylation of proteins. Usually, these enzymes add sugars to the hydroxyl groups of selected serine or threonine residues to form O-linked glycans or the amino groups of asparagine residues to form N-linked glycans. Different positions on the same polypeptide chain can contain differently linked glycans.
Multiple sugar molecules that may or may...
2.8K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Beyond α-GalCer: Medicinal Chemistry Insights Driving Structural Evolution of CD1d Ligands.

Journal of medicinal chemistry·2026
Same author

A kinetic trap mechanism underlies hHv1 inhibition by NZ-58.

The Journal of general physiology·2026
Same author

β-1,4-galactosyltransferase 1 inhibitors modulate cellular N-glycan profiles.

Biotechnology progress·2026
Same author

Mitochondria-Targeting Moieties Based on N-Tethered Pyridinium Cations.

Angewandte Chemie (International ed. in English)·2026
Same author

Probing Immune Signatures of Conjugated Pattern Recognition Receptor Ligands Identifies Chimeras with Potent Adjuvant and Antitumor Activities.

Journal of medicinal chemistry·2026
Same author

An Orally Available Halothiazole Glycomimetic as a Cancer-Targeting Dual Galectin-1 and Galectin-3 Inhibitor.

Journal of medicinal chemistry·2026

Related Experiment Video

Updated: Jun 17, 2025

Bioinformatics Resources for the Study of Glycan-Mediated Protein Interactions
11:21

Bioinformatics Resources for the Study of Glycan-Mediated Protein Interactions

Published on: January 20, 2022

3.3K

Galectin-8N-Selective 4-Halophenylphthalazinone-Galactals Double π-Stack in a Unique Pocket.

Sjors van Klaveren1,2, Mujtaba Hassan1, Maria Håkansson3

  • 1Department of Chemistry, Faculty of Science, Lund University, Naturvetarvägen 14, 223 62, Lund, Sweden.

ACS Medicinal Chemistry Letters
|August 14, 2024
PubMed
Summary

Researchers developed selective inhibitors for galectin-8, a protein with two carbohydrate recognition domains (CRDs). These novel glycomimetic-heterocycle hybrids show promise for studying galectin-8 biology and potential therapeutic applications.

More Related Videos

Characterization of Glycoproteins with the Immunoglobulin Fold by X-Ray Crystallography and Biophysical Techniques
08:58

Characterization of Glycoproteins with the Immunoglobulin Fold by X-Ray Crystallography and Biophysical Techniques

Published on: July 5, 2018

12.6K
Imaging Molecular Adhesion in Cell Rolling by Adhesion Footprint Assay
08:24

Imaging Molecular Adhesion in Cell Rolling by Adhesion Footprint Assay

Published on: September 27, 2021

3.1K

Related Experiment Videos

Last Updated: Jun 17, 2025

Bioinformatics Resources for the Study of Glycan-Mediated Protein Interactions
11:21

Bioinformatics Resources for the Study of Glycan-Mediated Protein Interactions

Published on: January 20, 2022

3.3K
Characterization of Glycoproteins with the Immunoglobulin Fold by X-Ray Crystallography and Biophysical Techniques
08:58

Characterization of Glycoproteins with the Immunoglobulin Fold by X-Ray Crystallography and Biophysical Techniques

Published on: July 5, 2018

12.6K
Imaging Molecular Adhesion in Cell Rolling by Adhesion Footprint Assay
08:24

Imaging Molecular Adhesion in Cell Rolling by Adhesion Footprint Assay

Published on: September 27, 2021

3.1K

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Structural Biology

Background:

  • Galectin-8 possesses two distinct carbohydrate recognition domains (CRDs).
  • Targeted inhibition of specific CRDs is crucial for understanding galectin-8 functions and developing therapeutics.

Purpose of the Study:

  • To design and discover potent and selective inhibitors targeting galectin-8's carbohydrate recognition domains.
  • To develop tool compounds for galectin-8 biology studies and potential drug development.

Main Methods:

  • Structure-guided design of glycomimetic-heterocycle hybrid ligands.
  • Biochemical assays to determine binding affinity (Kd) and selectivity against various galectins.
  • X-ray crystallography to elucidate ligand-protein interactions at high resolution (1.30 Å).
  • In vitro ADME (Absorption, Distribution, Metabolism, Excretion) studies including LogD, permeability, and stability assessments.

Main Results:

  • A 4-(p-bromophenyl)phthalazinone derivative demonstrated a 34 μM Kd for galectin-8N (N-terminal CRD).
  • This compound exhibited high selectivity, showing no binding to galectin-8C and other tested galectins, with >40-fold selectivity over galectin-4C.
  • X-ray structure revealed specific interactions within the galectin-8N-specific sub-pocket, explaining the observed selectivity.
  • Favorable physicochemical properties (LogD) and good passive permeability were observed.
  • Promising chemical, microsomal, and plasma stability were confirmed.

Conclusions:

  • Novel glycomimetic-heterocycle hybrids are potent and selective inhibitors of galectin-8N.
  • The identified compounds serve as valuable tool compounds for galectin-8 research.
  • These molecules represent promising candidates for hit-to-lead optimization in drug discovery.