Targeting Bacterial Sortase A with Covalent Inhibitors: 27 New Starting Points for Structure-Based Hit-to-Lead Optimization.
Aminoacyltransferases
/ antagonists & inhibitors
Animals
Anti-Bacterial Agents
/ chemistry
Bacterial Proteins
/ antagonists & inhibitors
Binding Sites
Catalytic Domain
Cysteine Endopeptidases
Drug Discovery
Fibroblasts
/ drug effects
Magnetic Resonance Spectroscopy
Mice
Molecular Docking Simulation
NIH 3T3 Cells
Small Molecule Libraries
Staphylococcus aureus
/ drug effects
Virulence Factors
/ antagonists & inhibitors
3-hydroxy-4H-pyran-4-one
NMR spectroscopy
antivirulence drugs
covalent inhibitors
sortase A
Journal
ACS infectious diseases
ISSN: 2373-8227
Titre abrégé: ACS Infect Dis
Pays: United States
ID NLM: 101654580
Informations de publication
Date de publication:
14 02 2020
14 02 2020
Historique:
pubmed:
15
11
2019
medline:
12
1
2021
entrez:
15
11
2019
Statut:
ppublish
Résumé
Because of its essential role as a bacterial virulence factor, enzyme sortase A (SrtA) has become an attractive target for the development of new antivirulence drugs against Gram-positive infections. Here we describe 27 compounds identified as covalent inhibitors of
Identifiants
pubmed: 31724850
doi: 10.1021/acsinfecdis.9b00265
doi:
Substances chimiques
Anti-Bacterial Agents
0
Bacterial Proteins
0
Small Molecule Libraries
0
Virulence Factors
0
Aminoacyltransferases
EC 2.3.2.-
sortase A
EC 2.3.2.-
Cysteine Endopeptidases
EC 3.4.22.-
Types de publication
Letter
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM