Selective Monovalent Galectin-8 Ligands Based on 3-Lactoylgalactoside
(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.
(Less)
- author
- organization
- publishing date
- 2022
- 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}}, }