Inhibitors of translation targeting eukaryotic translation initiation factor 4A.
The RNA helicases eIF4AI and eIF4AII play key roles in recruiting ribosomes to mRNA templates during eukaryotic translation initiation. Small molecule inhibitors of eIF4AI and eIF4AII have been useful for chemically dissecting their role in translation in vitro and in vivo. Here, we describe a screen performed on a small focused library of kinase inhibitors to identify a novel helicase inhibitor. We describe assays that have been critical for characterizing novel RNA helicase inhibitors.
Department of Biochemistry, McGill University, Montreal, Quebec, Canada.
Regina
R
Cencic
Gabriela
G
Galicia-Vázquez
Jerry
J
Pelletier
D000818:Animals; D000873:Anthracenes; D001572:Benzofurans / Q000494:pharmacology; D004852:Epoxy Compounds / Q000494:pharmacology; D039601:Eukaryotic Initiation Factor-4A / Q000037:antagonists & inhibitors*; D006801:Humans; D018942:Macrolides / Q000494:pharmacology; D010569:Perylene / Q000031:analogs & derivatives / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D013261:Sterols / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology
D000873:Anthracenes; D001572:Benzofurans; D004852:Epoxy Compounds; D018942:Macrolides; D047428:Protein Kinase Inhibitors; D013261:Sterols; D013844:Thiazoles; C510125:hippuristanol; C421324:pateamine A; D010569:Perylene; C004965:hypericin; C107772:rocaglamide; D039601:Eukaryotic Initiation Factor-4A