title: Synthesis of biotinylated episilvestrol: highly selective targeting of the translation factors eIF4AI/II.
abstract: Silvestrol (1) and episilvestrol (2) are protein synthesis inhibitors, and the former has shown efficacy in multiple mouse models of cancer; however, the selectivity of these potent cytotoxic natural products has not been described. Herein, it is demonstrated that eukaryotic initiation factors eIF4AI/II were the only proteins detected to bind silvestrol (1) and biotinylated episilvestrol (9) by affinity purification. Our study demonstrates the remarkable selectivity of these promising chemotherapeutics.
authors: School of Chemistry, The Bio21 Institute, The University of Melbourne, Melbourne, Victoria 3010, Australia.
authors: Jennifer M
authors: JM
authors: Chambers
authors: Lisa M
authors: LM
authors: Lindqvist
authors: Andrew
authors: A
authors: Webb
authors: David C S
authors: DC
authors: Huang
authors: G Paul
authors: GP
authors: Savage
authors: Mark A
authors: MA
authors: Rizzacasa
mesh_terms: D000818:Animals; D019921:Biotinylation; D039601:Eukaryotic Initiation Factor-4A / Q000037:antagonists & inhibitors*; D006801:Humans; D051379:Mice; D011500:Protein Synthesis Inhibitors / Q000737:chemistry / Q000494:pharmacology; D014315:Triterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001572:Benzofurans
chemical_list: D039601:Eukaryotic Initiation Factor-4A; D011500:Protein Synthesis Inhibitors; D014315:Triterpenes; C489893:episilvestrol; C489897:silvestrol; D001572:Benzofurans