Structure-Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin.
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
13 08 2020
13 08 2020
Historique:
pubmed:
11
7
2020
medline:
26
11
2020
entrez:
11
7
2020
Statut:
ppublish
Résumé
High-throughput screening has shown that Retro-1 inhibits ricin and Shiga toxins by diminishing their intracellular trafficking via the retrograde route, from early endosomes to the Golgi apparatus. To improve the activity of Retro-1, a structure-activity relationship (SAR) study was undertaken and yielded an analogue with a roughly 70-fold better half-maximal effective concentration (EC
Identifiants
pubmed: 32648758
doi: 10.1021/acs.jmedchem.0c00298
doi:
Substances chimiques
7-bromo-5-phenyl-4-propionyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one
0
Benzodiazepinones
0
Shiga Toxins
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM