Glycomics for Drug Discovery: Metabolic Perturbation in Androgen-Independent Prostate Cancer Cells Induced by Unnatural Hexosamine Mimics


  • This work was partly supported by a grant for “Innovation COE Project for Future Medicine and Medical Research” from the Ministry of Education, Culture, Science, and Technology (Japan). We appreciate the assistance with the analysis of sugar nucleotides by Dr. Y. Takegawa of Hokkaido University.


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Inhibited: N-acetylglucosamine (GlcNAc) derivatives with a fluorine atom at the C4 position (24) were synthesized, and their ability to inhibit cancer-cell growth was investigated. The administration of these 4F-GlcNAc derivatives to cells led to the unnatural sugar nucleotide 1. Furthermore, N-glycan profiles of cells were determined by using a glycoblotting-based enrichment analysis, which is suitable for high-throughput screenings for drug discovery.