Search for Protein Farnesyltransferase Inhibitors of Microbial Origin: Our Strategy and Results as well as the Results Obtained by Other Groups

Shigeo Iwasaki; Satoshi Omura

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Search for Protein Farnesyltransferase Inhibitors of Microbial Origin: Our Strategy and Results as well as the Results Obtained by Other Groups

机译：搜索微生物来源的蛋白质法呢基转移酶抑制剂：我们的策略和结果以及其他团体获得的结果

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Mutant ras oncogenes are associated with various human tumors,being found in approximately 25% of all human cancers.Since its identification,the enzyme Ras protein farnesyltransferase (PFTase),which catalyzes the initial step of Ras-processing,has been viewed as a most promising target for cancer therapy.Consequently,a number of synthetic and natural small molecules have been searched and developed according to this concept during the 1990s.Among these,microbial metabolites have provided diverse structural classes of compounds which exhibit PFTase inhibitory activity.This article reviews our work on PFTase inhibitors originating from microbial metabolites,and the results of similar works carried out by several other research groups.

机译：突变的ras癌基因与各种人类肿瘤有关，大约占所有人类癌症的25％。自鉴定以来，催化Ras加工起始步骤的Ras蛋白法呢基转移酶（PFTase）被认为是最重要的。因此，在1990年代，根据这一概念已经研究和开发了许多合成的和天然的小分子。其中，微生物代谢物提供了多种具有PFTase抑制活性的化合物。我们对源自微生物代谢产物的PFTase抑制剂的研究，以及其他几个研究小组进行的类似研究的结果。

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《The Journal of Antibiotics: An International Journal》 |2007年第1期|共12页
作者
Shigeo Iwasaki; Satoshi Omura;
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正文语种 eng
中图分类药学;
关键词
inhibitor of protein farnesyltransferase; microbial metabolites; screening and assay system; gliotoxin; pepticinnamins; andrastins; kurasoins;

机译：蛋白法呢基转移酶抑制剂;微生物代谢产物;筛选和测定系统;胶质毒素;胃蛋白酶;andrastins;kurasoins;

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1. Search for Protein Farnesyltransferase Inhibitors of Microbial Origin: Our Strategy and Results as well as the Results Obtained by Other Groups [J] . Shigeo Iwasaki, Satoshi Omura The Journal of Antibiotics: An International Journal . 2007,第1期

机译：搜索微生物来源的蛋白质法呢基转移酶抑制剂：我们的策略和结果以及其他团体获得的结果
2. 3D-QSAR with the aid of pharmacophore search and docking-based alignments for farnesyltransferase inhibitors. [J] . Vaidya M, Weigt M, Wiese M European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第10期

机译：3D-QSAR借助药效基团搜索和法尼基转移酶抑制剂的基于对接的比对。
3. From peptide libraries to optimized nonpeptide ligands in the search for S-farnesyltransferase inhibitors. [J] . Henlin JM, Boutin JA, Kucharczyk N, The journal of peptide research: official journal of the American Peptide Society . 2001,第2期

机译：从肽库到优化的非肽配体，以寻找S-法呢基转移酶抑制剂。
4. Synthesis of new protein farnesyltransferase inhibitors(Abstracts) [C] . Jennifer Zeitouni, Renata Marcia de Figueiredo, Joelle Dubois European Symposium on Organic Chemistry . 2007

机译：新蛋白法扰酶抑制剂的合成（摘要）
5. Design, synthesis, and biological evaluation of molecules of medicinal interest: Inhibitors of mammalian and Trypanosoma cruzi protein farnesyltransferase and Trypanosoma cruzi lanosterol-14-alpha-demethylase. [D] . Lockman, Jeffrey William. 2003

机译：设计，合成和具有药用价值的分子的生物学评估：哺乳动物和克鲁斯锥虫蛋白法尼基转移酶和克鲁斯锥虫羊毛甾醇14-α-脱甲基酶的抑制剂。
6. Structures of Cryptococcus neoformans Protein Farnesyltransferase Reveal Strategies for Developing Inhibitors That Target Fungal Pathogens [O] . Michael A. Hast, Connie B. Nichols, Stephanie M. Armstrong, 2011

机译：新型隐球菌蛋白法尼基转移酶的结构揭示了针对真菌病原体的抑制剂开发策略。
7. Structures of Cryptococcus neoformans Protein Farnesyltransferase Reveal Strategies for Developing Inhibitors That Target Fungal Pathogens* [O] . Michael A. Hast, Connie B. Nichols, Stephanie M. Armstrong, 2011

机译：隐性球菌蛋白蛋白法蛋白质法虫转移酶的结构揭示了靶向真菌病原体的抑制剂的策略*

Search for Protein Farnesyltransferase Inhibitors of Microbial Origin: Our Strategy and Results as well as the Results Obtained by Other Groups

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