Physical and Theoretical Chemistry Laboratory, Department of Chemistry, University of Oxford, Oxford, OX1 3QZ, UK.
The Kavli Institute for Nanoscience Discovery, 3 South Parks Road, Oxford, OX1 3QU, UK.
Chem Commun (Camb). 2021 Oct 14;57(82):10747-10750. doi: 10.1039/d1cc04186j.
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.
我们开发了一种基于质谱的本土方法来定量 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一种抗菌肽和小分子破坏剂的效力和功效,从而获得有关它们结构-活性关系的新信息。这种方法导致了发现基于喹啉的命中化合物,为开发新型 LPS 转运抑制剂奠定了基础。