Analysis of 6-(2,2-Dichloroacetamido)chrysene Interaction with the Hypoxanthine Phosphoribosyltransferase from Trypanosoma cruzi

Francisco J. Medrano; Mary A. Wenck; Juan C. Engel; Sydney P. Craig III

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Analysis of 6-(2,2-Dichloroacetamido)chrysene Interaction with the Hypoxanthine Phosphoribosyltransferase from Trypanosoma cruzi

机译：克氏锥虫次黄嘌呤磷酸核糖基转移酶与6-（2,2-二氯乙酰胺基）ch相互作用的分析

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Selective inhibition is needed for drugs targeting the hypoxanthine phosphoribosyltransferase of Trypanosoma cruzi, etiologic agent of Chagas' disease. 6-(2,2-Dichloroacetamido)chrysene, was shown herein to be a selective inhibitor of the trypanosomal enzyme. SAR analysis revealed that the 6-amido moiety was essential, but the dichloroaceto moiety was not essential for achieving the low K_i for this inhibitor. Understanding the molecular basis for these interactions could facilitate the design of selective inhibitors without a chrysene moiety.

机译：对于靶向恰加斯氏病的病原体克氏锥虫次黄嘌呤磷酸核糖基转移酶的药物，需要选择性抑制。 6-（2,2-二氯乙酰胺基）ch在本文中显示是锥虫酶的选择性抑制剂。 SAR分析表明，6-酰胺基部分是必不可少的，但是二氯乙酰基部分对于实现该抑制剂的低K_i并不是必需的。理解这些相互作用的分子基础可以促进无without部分选择性抑制剂的设计。

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《Journal of Medicinal Chemistry》 |2003年第12期|共3页
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Francisco J. Medrano; Mary A. Wenck; Juan C. Engel; Sydney P. Craig III;
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1. Analysis of 6-(2,2-Dichloroacetamido)chrysene Interaction with the Hypoxanthine Phosphoribosyltransferase from Trypanosoma cruzi [J] . Francisco J. Medrano, Mary A. Wenck, Juan C. Engel, Journal of Medicinal Chemistry . 2003,第12期

机译：克氏锥虫次黄嘌呤磷酸核糖基转移酶与6-（2,2-二氯乙酰胺基）ch相互作用的分析
2. Saturation mutagenesis, complement selection, and steady-state kinetic studies illuminate the roles of invariant residues in active site loop I of the hypoxanthine phosphoribosyltransferase from Trypanosoma cruzi [J] . Aimee C. Butterworth, Francisco J. Medrano, Ann E. Eakin, Biochimica et biophysica acta: BBA: International journal of biochemistry, biophysics and molecular biololgy. Proteins and Proteomics . 2004,第1a2期

机译：饱和诱变，补体选择和稳态动力学研究阐明了不变残基在克鲁氏锥虫次黄嘌呤磷酸核糖基转移酶活性位点环Ⅰ中的作用。
3. A 1.4 A crystal structure for the hypoxanthine phosphoribosyltransferase of Trypanosoma cruzi [J] . Focia PJ, Craig SP III, Nieves Alicea R, Biochemistry . 1998,第43期

机译：1.4克氏锥虫次黄嘌呤磷酸核糖基转移酶的晶体结构
4. Study of optically trapped living Trypanosoma cruzi/Trypanosoma rangeli - Rhodnius prolixus interactions by real time confocal images using CdSe quantum dots [C] . A. A. de Thomaz, D. B. Almeida, W. M. Faustino, Conference on optical trapping and optical micromanipulation . 2008

机译：光学捕获的活锥虫瘤rangeli / rangli - rangnius rangeli - rangnius rangeli使用Cdse量子点的实时共焦图像相互作用
5. Expression and functional analysis of lipids and glycolipids from the mammal-dwelling stages of Trypanosoma cruzi [D] . Lopes, Felipe Gazos 2015

机译：克氏锥虫哺乳动物居住阶段脂质和糖脂的表达和功能分析
6. Hypoxanthine phosphoribosyltransferase from Trypanosoma cruzi as a target for structure-based inhibitor design: crystallization and inhibition studies with purine analogs. [O] . A E Eakin, A Guerra, P J Focia, 1997

机译：来自克氏锥虫的次黄嘌呤磷酸核糖基转移酶作为基于结构的抑制剂设计的目标：使用嘌呤类似物进行结晶和抑制研究。
7. Crystal structures and inhibition of Trypanosoma brucei hypoxanthine-guanine phosphoribosyltransferase [O] . Terán David, Hocková Dana, Česnek Michal, 2016

机译：布鲁氏锥虫次黄嘌呤-鸟嘌呤磷酸核糖基转移酶的晶体结构及其抑制

Analysis of 6-(2,2-Dichloroacetamido)chrysene Interaction with the Hypoxanthine Phosphoribosyltransferase from Trypanosoma cruzi

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