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Potent Inhibitors of Thioredoxin Glutathione Reductase: Grail of Anti-Schistosome Drug within Reach?
ACS Infectious Diseases ( IF 5.3 ) Pub Date : 2020-03-11 , DOI: 10.1021/acsinfecdis.0c00072
Timir Tripathi 1 , Purna B Chetri 1
Affiliation  

Species of the blood fluke Schistosoma are responsible for schistosomiasis, the second most common parasitic disease, which is prevalent particularly in poor communities. Under redox pressure, schistosomes survive in mammalian hosts with the help of thioredoxin glutathione reductase, which is an essential selenoenzyme. A recent study identified compounds with extremely potent antischistosome activity. Most importantly, certain compounds were active against all major schistosomes across different life cycle stages, where even praziquantel, the drug of choice, fails. The data offer compounds that exceed WHO standards for leads for schistosomiasis therapy activity. The work may serve as the basis for the development of new antischistosome compounds.

中文翻译:

硫氧还蛋白谷胱甘肽还原酶的有效抑制剂:抗血吸虫病药物的作用范围?

血吸虫血吸虫的种类是血吸虫病的原因,血吸虫病是第二大最常见的寄生虫病,在贫困社区尤其普遍。在氧化还原压力下,血吸虫在哺乳动物宿主中借助硫氧还蛋白谷胱甘肽还原酶(一种必不可少的硒酶)存活。最近的一项研究鉴定出具有极强抗血吸虫活性的化合物。最重要的是,某些化合物在不同生命周期阶段对所有主要血吸虫均具有活性,即使选择的药物吡喹酮也失效。数据提供的血药浓度超过世卫组织标准的血吸虫病治疗活性化合物。这项工作可以作为开发新的抗血吸虫体化合物的基础。
更新日期:2020-03-11
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