Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example,Journal of Medicinal Chemistry

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Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2018-04-13 00:00:00 , DOI: 10.1021/acs.jmedchem.8b00318
Yiyue Xie ₁ , Jayme L. Dahlin ₂ , Aaron J. Oakley ₃ , Marco G. Casarotto ₄ , Philip G. Board ₄ , Jonathan B. Baell _{1,

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Affiliation

Early stage drug discovery reporting on relatively new or difficult targets is often associated with insufficient hit triage. Literature reviews of such targets seldom delve into the detail required to critically analyze the associated screening hits reported. Here we take the enzyme glutathione transferase omega-1 (GSTO1-1) as an example of a relatively difficult target and review the associated literature involving small-molecule inhibitors. As part of this process we deliberately pay closer-than-usual attention to assay interference and hit quality aspects. We believe this Perspective will be a useful guide for future development of GSTO1-1 inhibitors, as well serving as a template for future review formats of new or difficult targets.

中文翻译：

审查困难目标的命中发现文献：谷胱甘肽转移酶Omega-1为例

关于相对较新或困难目标的早期药物发现报告通常与击中分类不足有关。对此类目标的文献综述很少深入研究批判性分析所报道的相关筛选命中所需的细节。在这里，我们以谷胱甘肽转移酶omega-1（GSTO1-1）为例作为一个相对困难的目标的例子，并回顾了涉及小分子抑制剂的相关文献。作为此过程的一部分，我们故意在分析干扰和命中质量方面给予比平时更近的关注。我们认为，此《观点》将为GSTO1-1抑制剂的未来开发提供有用的指导，并为新的或困难目标的未来审查格式提供模板。

更新日期：2018-04-13

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