Synthesis of Inhibitors against Glycosyltransferases

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  • 糖転移酵素に対する阻害剤の合成
  • トウ テンイ コウソ ニ タイスル ソガイザイ ノ ゴウセイ

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Inhibitors against glycosyltransferases and glycosidases, which build up oligosaccharide moieties of biologically active glycoconjugates, are essential tools for the development of glycobiology and promising candidates of novel agents for the treatments of tumors, inflammatory, autoimmune diseases, and bacterial and virus infections. Many excellent inhibitors against glycosidases, such as deoxynojirimycin and oseltamivir, were found from nature and developed by good combination of structural biology and synthetic chemistry. However, excellent inhibitors of glycosyltransferases have not been developed until recently, because of little information on the structures of active sites of the enzymes, involvement of several components in the transition state of the enzyme catalyzed reaction, low affinities between the enzymes and substrates, and no facile assay systems for the inhibitory activities. The strategies regarding the design and the synthesis of the inhibitors for glycosyltransferases have been remarkably advanced in the last five years. In this review, we summarize the current stage of the synthesis of inhibitors against glycosyltransferases.

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