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首页> 外文期刊>Acta crystallographica. Section D, Structural biology >Intracellular drug binding affinities by NMR
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Intracellular drug binding affinities by NMR

机译：细胞内药物由NMR结合亲和力

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Most small-molecule drugs fulfill their function in cells, but studying direct compoundtarget interactions in a cellular environment is challenging. Nevertheless, this is crucial information guiding drug development where drug engagement at the desired site of action and potential off-target binding and activity need to be assessed as early as possible. Rather than intracellular binding affinities, available approaches rely on activity-based cellular assays, and provide a downstream and indirect impact of the respective compounds on target activity. In 2006, several seminal publications proposed a first solution towards this problem by demonstrating that nuclear magnetic resonance (NMR) spectroscopy can be used to study proteins in living cells (Selenko et al., 2006; Serber et al., 2006). Since then, ‘in-cell NMR’ has been successfully applied to study proteins, their (post-translational) modifications and interactions (reviewed in Luchinat & Banci, 2017; Selenko & Wagner, 2007; Pastore & Temussi, 2017; Siegal & Selenko, 2019). More recently, several groups have shown that in-cell NMR can be used to study interactions of proteins with small-molecule compounds in living cells (DeMott et al., 2018; Luchinat et al., 2020). However, whether intracellular compound-target interactions can be determined quantitatively in terms of binding affinities has remained unknown.
机译：大多数小分子药物实现其功能在细胞,但直接compoundtarget学习相互作用在细胞环境中具有挑战性的。信息指导药物开发药物接触所需的行动和网站潜在的非目标绑定和活动需要尽可能早地进行评估。细胞内绑定相似,可用方法依赖于基于活动的细胞化验,并提供一个下游和间接各自的目标化合物的影响活动。对这个问题,提出了一个第一的解决方案证明核磁共振(NMR)光谱学可以用来研究蛋白质在活细胞(Selenko et al ., 2006;, 2006)。成功地应用于研究蛋白质,他们翻译后的修改和交互(综述Luchinat & Banci, 2017;Siegal & Selenko, 2019)。组织表明,NMR - sensing可以用来研究蛋白质的相互作用在活细胞(更小分子化合物et al ., 2018;细胞内是否compound-target交互可以定量确定绑定的关联性仍然未知。

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