Front Cover: Identification of Pyrrolidine‐3‐acetic Acid Derived Oximes as Potent Inhibitors of γ‐Aminobutyric Acid Transporter 1 through Library Screening with MS Binding Assays (ChemMedChem 23/2018),ChemMedChem

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Front Cover: Identification of Pyrrolidine‐3‐acetic Acid Derived Oximes as Potent Inhibitors of γ‐Aminobutyric Acid Transporter 1 through Library Screening with MS Binding Assays (ChemMedChem 23/2018)
ChemMedChem ( IF 3.6 ) Pub Date : 2018-12-04 , DOI: 10.1002/cmdc.201800740
Simone K. Huber ₁ , Georg Höfner ₁ , Klaus T. Wanner ₁

Affiliation

The Front Cover shows the concept of library screening with MS binding assays. The libraries are generated by a simple reaction of a building block (Σ) with reactants with complementary reactivity and varying structures (A–X). Upon subsequent incubation with the target mGAT1, library members (ΣA–ΣH, ΣI–ΣP, ΣQ–ΣX) are selected according to their affinity towards the target. Best binders of libraries (ΣA) are identified by monitoring the amount of liberated reporter ligand (Φ) through (ESI)–MS/MS. As demonstrated by the results, MS binding assays represent a powerful tool in library screening. Cover illustration by Dr. Jörg Pabel. More information can be found in the Full Paper by Klaus T. Wanner et al. on page 2488 in Issue 23, 2018 (DOI: 10.1002/cmdc.201800556).

中文翻译：

封面：通过MS结合分析筛选文库，鉴定了吡咯烷-3-乙酸衍生的肟作为γ-氨基丁酸转运蛋白1的强抑制剂（ChemMedChem 23/2018）

封面显示了通过MS结合测定进行文库筛选的概念。库是通过结构单元（Σ）与具有互补反应性和变化结构（A–X）的反应物的简单反应生成的。在随后与靶标mGAT1一起温育后，根据库成员（对靶标的亲和力）选择库成员（ΣA–ΣH，ΣI–ΣP，ΣQ–ΣX）。通过监测通过（ESI）–MS / MS释放的报告配体（Φ）的数量，可以确定文库的最佳结合物（ΣA）。结果表明，MS结合测定是文库筛选的有力工具。JörgPabel博士的封面插图。可以在Klaus T. Wanner等人的《全文》中找到更多信息。就在第23期，2018页2488（：10.1002 / cmdc.201800556 DOI）。

更新日期：2018-12-04

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