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Peterson, Kristoffer; Kumar, Rohit; Stenström, Olof; Verma, Priya; Verma, Prashant R; Håkansson, Maria; Kahl-Knutsson, Barbro; Zetterberg, Fredrik; Leffler, Hakon; Akke, Mikael; Logan, Derek T; Nilsson, Ulf J
Journal of medicinal chemistry, 02/2018, Letnik: 61, Številka: 3Journal Article
Symmetrical and asymmetrical fluorinated phenyltriazolyl-thiodigalactoside derivatives have been synthesized and evaluated as inhibitors of galectin-1 and galectin-3. Systematic tuning of the phenyltriazolyl-thiodigalactosides’ fluoro-interactions with galectin-3 led to the discovery of inhibitors with exceptional affinities (K d down to 1–2 nM) in symmetrically substituted thiodigalactosides as well as unsurpassed combination of high affinity (K d 7.5 nM) and selectivity (46-fold) over galectin-1 for asymmetrical thiodigalactosides by carrying one trifluorphenyltriazole and one coumaryl moiety. Studies of the inhibitor–galectin complexes with isothermal titration calorimetry and X-ray crystallography revealed the importance of fluoro-amide interaction for affinity and for selectivity. Finally, the high affinity of the discovered inhibitors required two competitive titration assay tools to be developed: a new high affinity fluorescent probe for competitive fluorescent polarization and a competitive ligand optimal for analyzing high affinity galectin-3 inhibitors with competitive isothermal titration calorimetry.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Vir: Osebne bibliografije
in: SICRIS
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