2. Academic Validation
  3. Synthesis of biotinylated episilvestrol: highly selective targeting of the translation factors eIF4AI/II

Synthesis of biotinylated episilvestrol: highly selective targeting of the translation factors eIF4AI/II

  • Org Lett. 2013 Mar 15;15(6):1406-9. doi: 10.1021/ol400401d.
Jennifer M Chambers 1,  Lisa M Lindqvist,  Andrew Webb,  David C S Huang,  G Paul Savage,  Mark A Rizzacasa
Affiliations

Affiliation

  • 1 School of Chemistry, The Bio21 Institute, The University of Melbourne, Melbourne, Victoria 3010, Australia.
PMID: 23461621 DOI: 10.1021/ol400401d
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.

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