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“双底物”类似物对克氏锥虫甘油醛-3-磷酸脱氢酶的选择性抑制作用

Selective inhibition of Trypanosoma cruzi GAPDH by "bi-substrate" analogues.

作者信息

Ladame Sylvain, Fauré Régis, Denier Colette, Lakhdar-Ghazal Faouzi, Willson Michèle

机构信息

University Chemical Laboratory, University of Cambridge, Cambridge CB2 1EW, UK.

出版信息

Org Biomol Chem. 2005 Jun 7;3(11):2070-2. doi: 10.1039/b504703j. Epub 2005 May 9.

DOI:10.1039/b504703j
PMID:15917890
Abstract

A new series of "bi-substrate" analogues have been synthesized as potential inhibitors of the glyceraldehyde-3-phosphate dehydrogenase and one lead compound has been identified that inhibits the enzyme from Trypanosoma cruzi with good affinity and very high (50-fold) specificity.

摘要

已经合成了一系列新的“双底物”类似物作为甘油醛-3-磷酸脱氢酶的潜在抑制剂,并且已经鉴定出一种先导化合物,它以良好的亲和力和非常高(50倍)的特异性抑制克氏锥虫的该酶。

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Selective inhibition of Trypanosoma cruzi GAPDH by "bi-substrate" analogues.“双底物”类似物对克氏锥虫甘油醛-3-磷酸脱氢酶的选择性抑制作用
Org Biomol Chem. 2005 Jun 7;3(11):2070-2. doi: 10.1039/b504703j. Epub 2005 May 9.
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Discovery of novel Trypanosoma cruzi glyceraldehyde-3-phosphate dehydrogenase inhibitors.新型克氏锥虫甘油醛-3-磷酸脱氢酶抑制剂的发现
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The development of an immobilized enzyme reactor containing glyceraldehyde-3-phosphate dehydrogenase from Trypanosoma cruzi: the effect of species' specific differences on the immobilization.含有克氏锥虫3-磷酸甘油醛脱氢酶的固定化酶反应器的研制:物种特异性差异对固定化的影响。
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Evidence for the two phosphate binding sites of an analogue of the thioacyl intermediate for the Trypanosoma cruzi glyceraldehyde-3-phosphate dehydrogenase-catalyzed reaction, from its crystal structure.来自克氏锥虫甘油醛-3-磷酸脱氢酶催化反应的硫代酰基中间体类似物的两个磷酸结合位点的晶体结构证据。
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Selective tight binding inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase via structure-based drug design.通过基于结构的药物设计获得的锥虫甘油醛-3-磷酸脱氢酶的选择性紧密结合抑制剂。
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Effects of organic solvents on the enzyme activity of Trypanosoma cruzi glyceraldehyde-3-phosphate dehydrogenase in calorimetric assays.有机溶剂在量热测定中对克氏锥虫甘油醛-3-磷酸脱氢酶酶活性的影响。
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Structural basis for selective inhibition of trypanosomatid glyceraldehyde-3-phosphate dehydrogenase: molecular docking and 3D QSAR studies.锥虫甘油醛-3-磷酸脱氢酶选择性抑制的结构基础:分子对接和三维定量构效关系研究
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Conformational changes in Leishmania mexicana glyceraldehyde-3-phosphate dehydrogenase induced by designed inhibitors.设计抑制剂诱导的墨西哥利什曼原虫甘油醛-3-磷酸脱氢酶的构象变化
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