Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design principles

IF 4.3 2区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY Chemical Communications Pub Date : 2024-09-13 DOI:10.1039/d4cc03106g
Javier Ramos-Soriano, Maisie Holbrow-Wilshaw, Eliza Hunt, Y. Jennifer Jiang, Pablo Penalver, Juan Carlos Morales, M. Carmen Galan
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引用次数: 0

Abstract

Novel strategies against parasitic infections are of great importance. Here we describe a G4 DNA ligand with subnanomolar antiparasitic activity against T. brucei and a remarkable selectivity index (IC50 MRC-5/T. brucei) of 2285-fold. We also correlate the impact of small structural changes to G4 binding activity and antiparasitic activity.
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探究偶氮苯 G-四链配体的结合和抗寄生虫功效,研究 G4 配体的设计原则
针对寄生虫感染的新策略非常重要。在这里,我们描述了一种 G4 DNA 配体,它对布氏杆菌具有亚纳摩尔抗寄生虫活性,选择性指数(IC50 MRC-5/T.brucei)高达 2285 倍。我们还研究了微小结构变化对 G4 结合活性和抗寄生虫活性的影响。
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来源期刊
Chemical Communications
Chemical Communications 化学-化学综合
CiteScore
8.60
自引率
4.10%
发文量
2705
审稿时长
1.4 months
期刊介绍: ChemComm (Chemical Communications) is renowned as the fastest publisher of articles providing information on new avenues of research, drawn from all the world''s major areas of chemical research.
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