Tuning the preference of thiodigalactoside-and lactosamine-based ligands to galectin-3 over galectin-1
H van Hattum, HM Branderhorst, EE Moret… - Journal of Medicinal …, 2013 - ACS Publications
Inhibitors for galectin-1 and-3 were synthesized from thiodigalactoside and lactosamine by
derivatization of the galactose C3. Introduction of 4-phenyl-1 H-1, 2, 3-triazol-1-yl …
derivatization of the galactose C3. Introduction of 4-phenyl-1 H-1, 2, 3-triazol-1-yl …
Systematic tuning of fluoro-galectin-3 interactions provides thiodigalactoside derivatives with single-digit nM affinity and high selectivity
K Peterson, R Kumar, O Stenström… - Journal of medicinal …, 2018 - ACS Publications
Symmetrical and asymmetrical fluorinated phenyltriazolyl-thiodigalactoside derivatives have
been synthesized and evaluated as inhibitors of galectin-1 and galectin-3. Systematic tuning …
been synthesized and evaluated as inhibitors of galectin-1 and galectin-3. Systematic tuning …
Discovery of selective and orally available galectin-1 inhibitors
FR Zetterberg, C Diehl, M Håkansson… - Journal of Medicinal …, 2023 - ACS Publications
A new series of orally available α-d-galactopyranosides with high affinity and specificity
toward galectin-1 have been discovered. High affinity and specificity were achieved by …
toward galectin-1 have been discovered. High affinity and specificity were achieved by …
Synthesis, structure–activity relationships, and in vivo evaluation of novel tetrahydropyran-based thiodisaccharide mimics as galectin-3 inhibitors
L Xu, RA Hartz, BR Beno, K Ghosh… - Journal of Medicinal …, 2021 - ACS Publications
Galectin-3 is a member of a family of β-galactoside-binding proteins. A substantial body of
literature reports that galectin-3 plays important roles in cancer, inflammation, and fibrosis …
literature reports that galectin-3 plays important roles in cancer, inflammation, and fibrosis …
Biophysical and structural characterization of mono/di-arylated lactosamine derivatives interaction with human galectin-3
C Atmanene, C Ronin, S Téletchéa, FM Gautier… - Biochemical and …, 2017 - Elsevier
Combination of biophysical and structural techniques allowed characterizing and
uncovering the mechanisms underlying increased binding affinity of lactosamine derivatives …
uncovering the mechanisms underlying increased binding affinity of lactosamine derivatives …
Thiodigalactoside–bovine serum albumin conjugates as high-potency inhibitors of galectin-3: an outstanding example of multivalent presentation of small molecule …
H Zhang, D Laaf, L Elling, RJ Pieters - Bioconjugate Chemistry, 2018 - ACS Publications
Galectin inhibitors are urgently needed to understand the mode of action and druggability of
different galectins, but potent and selective agents still evade researchers. Small-sized …
different galectins, but potent and selective agents still evade researchers. Small-sized …
Aminopyrimidine–galactose hybrids are highly selective galectin-3 inhibitors
A Dahlqvist, FR Zetterberg, H Leffler, UJ Nilsson - MedChemComm, 2019 - pubs.rsc.org
Galectins are a family of carbohydrate recognition proteins involved in, among other things,
modulating cell signalling and cell–environment interactions, giving them roles in several …
modulating cell signalling and cell–environment interactions, giving them roles in several …
1H-1, 2, 3-triazol-1-yl thiodigalactoside derivatives as high affinity galectin-3 inhibitors
BA Salameh, I Cumpstey, A Sundin, H Leffler… - Bioorganic & medicinal …, 2010 - Elsevier
Galactose C3-triazole derivatives were synthesized by Cu (I)-catalyzed cycloaddition
between acetylenes and galactose C3-azido derivatives. Evaluation against galectin-3, 7 …
between acetylenes and galactose C3-azido derivatives. Evaluation against galectin-3, 7 …
Low Micromolar Inhibitors of Galectin‐3 Based on 3′‐Derivatization of N‐Acetyllactosamine
P Sörme, Y Qian, PG Nyholm, H Leffler… - …, 2002 - Wiley Online Library
A strategy for generating potential galectin inhibitors was devised based on derivatization at
the C‐3′ atom in 3′‐amino‐N‐acetyllactosamine by using structural knowledge of the …
the C‐3′ atom in 3′‐amino‐N‐acetyllactosamine by using structural knowledge of the …
Structure-Guided Design of d-Galactal Derivatives with High Affinity and Selectivity for the Galectin-8 N-Terminal Domain
M Hassan, F Baussière, S Guzelj… - ACS medicinal …, 2021 - ACS Publications
Galectin-8 is a carbohydrate-binding protein that plays a crucial role in tumor progression
and metastasis, antibacterial autophagy, modulation of the immune system, and bone …
and metastasis, antibacterial autophagy, modulation of the immune system, and bone …