Novel multisubstrate inhibitors of mammalian purine nucleoside phosphorylase.

Toms AV; Wang W; Li YGanem BEalick SE

首页> 外文期刊>Acta crystallographica.Section D. Biological crystallography >Novel multisubstrate inhibitors of mammalian purine nucleoside phosphorylase.

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Novel multisubstrate inhibitors of mammalian purine nucleoside phosphorylase.

机译：哺乳动物的小说multisubstrate抑制剂嘌呤核苷磷酸化酶。

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In an effort to develop potent multisubstrate-analog inhibitors of purine nucleoside phosphorylase (PNP), three nucleoside phosphonates were designed utilizing structural information from the previously reported structures of complexes of bovine PNP with substrates and products. The nucleoside phosphonates contain an acetal linkage at the O2' and O3' positions and a two-C-atom spacer between the ribose and phosphate moieties. The linkage enables the compounds to simultaneously occupy the purine-, ribose- and phosphate-binding sites. The chemical syntheses, inhibition profiles and structural characterization of these novel multisubstrate analog inhibitors with bovine PNP are described.

机译：为了有效发展multisubstrate-analog嘌呤的抑制剂核苷磷酸化酶(PNP),三个核苷为利用结构设计来自之前报道的信息配合物结构的牛PNP型基板和产品。为包含一个缩醛键O2的和O3的位置two-C-atom之间的间隔核糖和磷酸根。使化合物同时占领嘌呤-核糖,phosphate-binding网站。化学合成,抑制概要文件和这些小说的结构特征multisubstrate模拟与牛PNP型抑制剂描述。

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来源
《Acta crystallographica.Section D. Biological crystallography》 |2005年第11期|1449-1458|共10页
作者
Toms AV; Wang W; Li YGanem BEalick SE;
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作者单位

Department of Chemistry and Chemical Biology, Cornell University, Ithaca, NY 14853, USA.;

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原文格式 PDF
正文语种英语
中图分类化学;
关键词
Ribose; Purine Nucleoside Phosphorylase; Phosphonatesinorganic phosphate;

机译：核糖;嘌呤核苷磷酸化酶;Phosphonatesinorganic磷酸;

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Novel multisubstrate inhibitors of mammalian purine nucleoside phosphorylase.

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