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Selective Monovalent Galectin-8 Ligands Based on 3-Lactoylgalactoside

Girardi, Benedetta ; Manna, Martina ; Van Klaveren, Sjors LU ; Tomašič, Tihomir ; Jakopin, Žiga ; Leffler, Hakon LU ; Nilsson, Ulf J. LU ; Ricklin, Daniel ; Mravljak, Janez and Schwardt, Oliver , et al. (2022) In ChemMedChem 17(3).
Abstract

Galectin-8 has gained attention as a potential new pharmacological target for the treatment of various diseases, including cancer, inflammation, and disorders associated with bone mass reduction. To that end, new molecular probes are needed in order to better understand its role and its functions. Herein we aimed to improve the affinity and target selectivity of a recently published galectin-8 ligand, 3-O-[1-carboxyethyl]-β-d-galactopyranoside, by introducing modifications at positions 1 and 3 of the galactose. Affinity data measured by fluorescence polarization show that the most potent compound reached a KD of 12 μM. Furthermore, reasonable selectivity versus other galectins was achieved, making the highlighted compound a... (More)

Galectin-8 has gained attention as a potential new pharmacological target for the treatment of various diseases, including cancer, inflammation, and disorders associated with bone mass reduction. To that end, new molecular probes are needed in order to better understand its role and its functions. Herein we aimed to improve the affinity and target selectivity of a recently published galectin-8 ligand, 3-O-[1-carboxyethyl]-β-d-galactopyranoside, by introducing modifications at positions 1 and 3 of the galactose. Affinity data measured by fluorescence polarization show that the most potent compound reached a KD of 12 μM. Furthermore, reasonable selectivity versus other galectins was achieved, making the highlighted compound a promising lead for the development of new selective and potent ligands for galectin-8 as molecular probes to examine the protein's role in cell-based and in vivo studies.

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organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
carbohydrates, fluorescence polarization, galectin-8, galectins, molecular probes
in
ChemMedChem
volume
17
issue
3
publisher
Wiley-Blackwell
external identifiers
  • scopus:85116448380
  • pmid:34613662
ISSN
1860-7179
DOI
10.1002/cmdc.202100514
language
English
LU publication?
yes
additional info
Publisher Copyright: © 2021 Wiley-VCH GmbH
id
7f69e48a-47dc-44a6-8b69-7411a228fa24
date added to LUP
2021-10-25 14:30:00
date last changed
2024-06-15 19:16:13
@article{7f69e48a-47dc-44a6-8b69-7411a228fa24,
  abstract     = {{<p>Galectin-8 has gained attention as a potential new pharmacological target for the treatment of various diseases, including cancer, inflammation, and disorders associated with bone mass reduction. To that end, new molecular probes are needed in order to better understand its role and its functions. Herein we aimed to improve the affinity and target selectivity of a recently published galectin-8 ligand, 3-O-[1-carboxyethyl]-β-d-galactopyranoside, by introducing modifications at positions 1 and 3 of the galactose. Affinity data measured by fluorescence polarization show that the most potent compound reached a K<sub>D</sub> of 12 μM. Furthermore, reasonable selectivity versus other galectins was achieved, making the highlighted compound a promising lead for the development of new selective and potent ligands for galectin-8 as molecular probes to examine the protein's role in cell-based and in vivo studies.</p>}},
  author       = {{Girardi, Benedetta and Manna, Martina and Van Klaveren, Sjors and Tomašič, Tihomir and Jakopin, Žiga and Leffler, Hakon and Nilsson, Ulf J. and Ricklin, Daniel and Mravljak, Janez and Schwardt, Oliver and Anderluh, Marko}},
  issn         = {{1860-7179}},
  keywords     = {{carbohydrates; fluorescence polarization; galectin-8; galectins; molecular probes}},
  language     = {{eng}},
  number       = {{3}},
  publisher    = {{Wiley-Blackwell}},
  series       = {{ChemMedChem}},
  title        = {{Selective Monovalent Galectin-8 Ligands Based on 3-Lactoylgalactoside}},
  url          = {{http://dx.doi.org/10.1002/cmdc.202100514}},
  doi          = {{10.1002/cmdc.202100514}},
  volume       = {{17}},
  year         = {{2022}},
}