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糖组学在药物研发中的应用：非天然己糖类似物诱导雄激素非依赖性前列腺癌细胞的代谢紊乱。

Glycomics for drug discovery: metabolic perturbation in androgen-independent prostate cancer cells induced by unnatural hexosamine mimics.

机构信息

Graduate School of Advanced Life Science, Hokkaido University, Kita-ku, Sapporo, Japan.

出版信息

Angew Chem Int Ed Engl. 2012 Apr 2;51(14):3386-90. doi: 10.1002/anie.201108742. Epub 2012 Feb 17.

DOI:10.1002/anie.201108742
PMID:22345046
Abstract

Inhibited: N-acetylglucosamine (GlcNAc) derivatives with a fluorine atom at the C4 position (2-4) 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.

摘要

被抑制的

在 C4 位置（2-4）带有氟原子的 N-乙酰葡萄糖胺（GlcNAc）衍生物被合成出来，并研究了它们抑制癌细胞生长的能力。这些 4F-GlcNAc 衍生物被施用于细胞后，导致了非天然糖核苷酸 1 的产生。此外，使用基于糖印迹的富集分析来确定细胞的 N-聚糖图谱，这适用于药物发现的高通量筛选。

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