期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 20, 期 15, 页码 -出版社
MDPI
DOI: 10.3390/ijms20153786
关键词
galectin-1; gulopyranosides; fluorescence polarization; benzamide; selective
资金
- Swedish Research Council [621-2016-03667]
- Knut and Alice Wallenberg Foundation [KAW 2013.0022]
- Galecto Biotech AB, Sweden
Galectins are a family of galactoside-recognizing proteins involved in different galectin-subtype-specific inflammatory and tumor-promoting processes, which motivates the development of inhibitors that are more selective galectin inhibitors than natural ligand fragments. Here, we describe the synthesis and evaluation of 3-C-methyl-gulopyranoside derivatives and their evaluation as galectin inhibitors. Methyl 3-deoxy-3-C-(hydroxymethyl)-beta-d-gulopyranoside showed 7-fold better affinity for galectin-1 than the natural monosaccharide fragment analog methyl beta-d-galactopyranoside, as well as a high selectivity over galectin-2, 3, 4, 7, 8, and 9. Derivatization of the 3-C-hydroxymethyl into amides gave gulosides with improved selectivities and affinities; methyl 3-deoxy-3-C-(methyl-2,3,4,5,6-pentafluorobenzamide)-beta-d-gulopyranoside had K-d 700 mu M for galectin-1, while not binding any other galectin.
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