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研究领域生物医学和临床科学药理学和制药科学药物基因组学
作为Plasmodium Falciparum 6-Oxopurine Phosphoribosyltransferase的抑制剂的C1'-分支的环状核酸酸盐

作为Plasmodium Falciparum 6-Oxopurine Phosphoribosyltransferase的抑制剂的C1'-分支的环状核酸酸盐

Jan Frydrych ¹, Dianne T Keough ², Haojun Xia ², Lenka Poštová Slavětínská ¹, Martin Dračínský ¹, Michal Česnek ¹, Jye Travis ³, Marina Chavchich ³, Michael Edstein ³, Dana Hocková ¹, Luke W Guddat ², Zlatko Janeba ¹

Jan Frydrych ¹, Dianne T Keough ², Haojun Xia ²

¹Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 160 00, Prague 6, Czech Republic.
²School of Chemistry and Molecular Biosciences, The University of Queensland, Brisbane, 4072, Australia.
³Department of Drug Evaluation, Australian Defence Force Malaria and Infectious Disease Institute, Enoggera, Brisbane, Queensland, 4051, Australia.

⁰Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 160 00, Prague 6, Czech Republic.

Chemmedchem +

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2025年八月22日

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在PubMed上查看摘要

概括

此摘要是机器生成的。

基于纯素的新化合物显示出作为酸转移酶 (HGXPRT) 抑制剂的前景. 这些HGXPRT抑制剂可以治疗寄生虫感染和三阴性乳腺癌.

科学领域

医学化学
药物发现
寄生虫学

背景情况

低氨酸氨酸转移酶 (HGXPRT) 是对寄生虫感染和依赖MYC的三阴性乳腺癌的验证药物标.
目前的抑制剂策略涉及模仿过渡状态或产品类型.

研究的目的

设计和合成新型基于纯素的C1'-分支的非循环核酸酸盐作为潜在的HGXPRT抑制剂.
评估这些化合物对人类和Plasmodium falciparum HGXPRT的抑制活性.

主要方法

用各种二次链接剂合成基于纯素的C1'-分支的环形核酸酸盐.
酶抑制测定用于确定人类和Plasmodium falciparum HGXPRT的K<sub>i</sub>值.
在体外测试二胺酸原药对菌.

主要成果

几种化合物表现出对人类和Plasmodium falciparum HGXPRT的微小到低微小抑制活性.
获得的最低K< sub>i</ sub>值为人类HGXPRT的0. 7μM和Plasmodium falciparumHGXPRT的0. 4μM.
一种二胺原药的IC<sub>50</sub>为4. 3μM,对一种对药物敏感的Plasmodium falciparum菌株.

结论

基于氨酸的C1'-分支的非循环核酸酸是HGXPRT的有效抑制剂.
这些化合物为开发新的抗寄生虫和抗癌疗法提供了前景.
进一步优化C1'二次链接器对于增强抑制功效至关重要.

关键词:

虫非循环核酸酸盐停靠低氨酸-氨酸-氨酸) 基转移酶抑制剂疟疾

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Biosynthesis of Nucleic Acids

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Nucleic acid biosynthesis is a fundamental biochemical process that produces the purine and pyrimidine nucleotides essential for DNA and RNA synthesis. This pathway maintains a balanced nucleotide pool, preventing imbalances that could jeopardize genetic integrity and cellular function. Given the crucial role of nucleotides, their synthesis is tightly regulated to ensure proper cellular homeostasis.Purine BiosynthesisThe biosynthesis of purine nucleotides begins with ribose-5-phosphate, a...

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