Phenotypic Screening of Histone Deacetylase (HDAC) Inhibitors against Schistosoma mansoni,ChemMedChem

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Phenotypic Screening of Histone Deacetylase (HDAC) Inhibitors against Schistosoma mansoni
ChemMedChem ( IF 3.6 ) Pub Date : 2022-08-19 , DOI: 10.1002/cmdc.202100622
Muhammad Murtaza Hassan _{1,

2} , Abootaleb Sedighi _{1,

2} , Olasunkanmi O Olaoye _{1,

2} , Cécile Häberli _{3,

4} , Annika Merz ₅ , Elizabeth Ramos-Morales _{6,

7} , Elvin D de Araujo ₁ , Christophe Romier _{6,

7} , Manfred Jung ₅ , Jennifer Keiser _{3,

4} , Patrick T Gunning _{1,

2}

Affiliation

Recent literature has proposed HDAC8 as a potentially viable target for the treatment of schistosomiasis, a parasitic disease caused by the Schistosoma genus of blood flukes. This study highlights the applicability of a benzanilide-based histone deacetylase (HDAC) inhibitor library consisting of varying HDAC isozyme inhibition potencies and selectivities, to Schistosoma mansoni. This library was generated from a focused structure–activity relationship study on HDAC8 and shows no direct correlation between hHDAC8/SmHDAC8 potency and S. mansoni activity.

中文翻译：

针对曼氏血吸虫的组蛋白脱乙酰酶 (HDAC) 抑制剂的表型筛选

最近的文献提出HDAC8 作为治疗血吸虫病的潜在可行靶点，血吸虫病是一种由血吸虫属引起的寄生虫病。本研究强调了基于苯苯胺的组蛋白脱乙酰酶 (HDAC) 抑制剂库对曼氏血吸虫的适用性，该库由不同的 HDAC 同工酶抑制效力和选择性组成。该文库是从对 HDAC8 的集中结构-活性关系研究中生成的，并且显示 hHDAC8/SmHDAC8 效力与S. mansoni活性之间没有直接相关性。

更新日期：2022-08-19

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