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- W1966026530 abstract "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 galectin carbohydrate recognition site. A collection of 12 compounds was prepared by N-acylations or N-sulfonylations. Hydrophobic tagging of the O-3 atom in the N-acetylglucosamine residue with a stearic ester allowed rapid and simple product purification. The compounds were screened in a galectin-3 binding assay and three compounds with significantly higher inhibitory activities compared to the parent N-acetyllactosaminide were found. These three best inhibitors all carried an aromatic amide at the C-3' position of the galactose moiety, which indicates that favorable interactions were formed between the aromatic group and galectin-3. The best inhibitor had an IC50 value (4.4 microM) about 50 times better than the parent N-acetyllactosaminide, which implies that it has potential as a valuable tool for studying galectin-3 biological functions and also as a lead compound for the development of galectin-3-blocking pharmaceuticals." @default.
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- W1966026530 date "2002-03-01" @default.
- W1966026530 modified "2023-09-27" @default.
- W1966026530 title "Low Micromolar Inhibitors of Galectin‐3 Based on 3′‐Derivatization of<i>N</i>‐Acetyllactosamine" @default.
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- W1966026530 doi "https://doi.org/10.1002/1439-7633(20020301)3:2/3<183::aid-cbic183>3.0.co;2-#" @default.
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