Mass spectrometry enables the discovery of inhibitors of an LPS transport assembly
Anti-Infective Agents
/ chemistry
Crystallization
High-Throughput Screening Assays
Humans
Lipopolysaccharide Receptors
/ chemistry
Mass Spectrometry
/ methods
Oxazines
/ chemistry
Peptides
/ chemistry
Protein Binding
Protein Multimerization
Quinolines
/ chemistry
Small Molecule Libraries
/ chemistry
Structure-Activity Relationship
Journal
Chemical communications (Cambridge, England)
ISSN: 1364-548X
Titre abrégé: Chem Commun (Camb)
Pays: England
ID NLM: 9610838
Informations de publication
Date de publication:
14 Oct 2021
14 Oct 2021
Historique:
pubmed:
30
9
2021
medline:
15
12
2021
entrez:
29
9
2021
Statut:
epublish
Résumé
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.
Identifiants
pubmed: 34585198
doi: 10.1039/d1cc04186j
pmc: PMC7614387
mid: EMS172723
doi:
Substances chimiques
Anti-Infective Agents
0
Lipopolysaccharide Receptors
0
Oxazines
0
Peptides
0
Quinolines
0
Small Molecule Libraries
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
10747-10750Subventions
Organisme : Medical Research Council
ID : MR/V028839/1
Pays : United Kingdom
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