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Acyclic nucleoside phosphonates as possible chemotherapeutics against Trypanosoma brucei.
Drug Discovery Today ( IF 6.5 ) Pub Date : 2020-03-02 , DOI: 10.1016/j.drudis.2020.02.008
David Terán 1
Affiliation  

Human African trypanosomiasis is a life-threatening illness caused by Trypanosoma brucei. Owing to the toxic side effects of the available therapeutics, new medications for this disease are needed. One potential drug target is the 6-oxopurine phosphoribosyltransferases (PRTs), the activity of which is crucial to produce purine nucleotide monophosphates required for DNA and RNA synthesis. Inhibitors of the 6-oxopurine PRTs that show promising results as drug leads are the acyclic nucleoside phosphonates (ANPs). ANPs are very flexible in their structure, enabling important conformational changes to facilitate the binding of this class of compounds in the active site of the 6-oxopurine PRTs.



中文翻译:

无环核苷膦酸盐作为可能的抗布氏锥虫的化学治疗剂。

非洲人类锥虫病是一种由布氏锥虫引起的危及生命的疾病。由于现有疗法的毒副作用,需要针对这种疾病的新药物。一个潜在的药物靶点是 6-氧代嘌呤磷酸核糖基转移酶 (PRT),其活性对于产生 DNA 和 RNA 合成所需的嘌呤核苷酸单磷酸酯至关重要。6-氧代嘌呤 PRTs 的抑制剂是无环核苷膦酸盐 (ANPs),作为药物先导药物显示出有希望的结果。ANP 的结构非常灵活,能够进行重要的构象变化,以促进此类化合物在 6-氧嘌呤 PRT 的活性位点的结合。

更新日期:2020-03-02
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