Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase.
Animals
Benzofurans
/ chemistry
Binding Sites
Breast Neoplasms
/ drug therapy
Cell Line, Tumor
Crystallography, X-Ray
Drug Design
Eukaryotic Initiation Factor-4A
/ antagonists & inhibitors
Female
Half-Life
Humans
Ligands
Mice
Mice, Nude
Molecular Dynamics Simulation
Mutagenesis, Site-Directed
Protein Structure, Tertiary
RNA, Messenger
/ chemistry
Rats
Structure-Activity Relationship
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:
11 06 2020
11 06 2020
Historique:
pubmed:
30
5
2020
medline:
13
11
2020
entrez:
30
5
2020
Statut:
ppublish
Résumé
Dysregulation of protein translation is a key driver for the pathogenesis of many cancers. Eukaryotic initiation factor 4A (eIF4A), an ATP-dependent DEAD-box RNA helicase, is a critical component of the eIF4F complex, which regulates cap-dependent protein synthesis. The flavagline class of natural products (
Identifiants
pubmed: 32470302
doi: 10.1021/acs.jmedchem.0c00182
doi:
Substances chimiques
Benzofurans
0
Ligands
0
RNA, Messenger
0
Eukaryotic Initiation Factor-4A
EC 2.7.7.-
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM