Mass spectrometry enables the discovery of inhibitors of an LPS transport assembly via disruption of protein-protein interactions.

Mass spectrometry enables the discovery of inhibitors of an LPS transport assembly via disruption of protein-protein interactions.
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DOI:
10.1039/d1cc04186j
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发表时间:
2021-10-14
期刊:
Chemical communications (Cambridge, England)
影响因子:
--
通讯作者:
Robinson CV
Robinson CV
中科院分区:
其他
文献类型:
--
作者:
Fiorentino F;Rotili D;Mai A;Bolla JR;Robinson CV

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我们开发了一种基于天然质谱的方法来量化 LPS 转运蛋白 LptH 的单体-二聚体平衡。我们使用这种方法来评估抗菌肽和小分子干扰物的效力和功效,获得有关其结构-活性关系的新信息。这种方法导致了基于喹啉的命中化合物的鉴定,这为开发新型 LPS 转运抑制剂奠定了基础。
We developed a native mass spectrometry-based approach to quantify the monomer–dimer equilibrium of the LPS transport protein LptH. We use this method to assess the potency and efficacy of an antimicrobial peptide and small molecule disruptors, obtaining new information on their structure–activity relationships. This approach led to the identification of quinoline-based hit compounds representing the basis for the development of novel LPS transport inhibitors.
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