A comparative study of small molecules targeting eIF4A

Sai Kiran Naineni, Rayelle Itoua Maïga, Regina Cencic, Andrea A. Putnam, Luis A. Amador, Abimael D. Rodriguez, Eckhard Jankowsky, Jerry Pelletier

Research output: Contribution to journalArticlepeer-review


The PI3K/Akt/mTOR kinase pathway is extensively deregulated in human cancers. One critical node under regulation of this signaling axis is eukaryotic initiation factor (eIF) 4F, a complex involved in the control of translation initiation rates. eIF4F-dependent addictions arise during tumor initiation and maintenance due to increased eIF4F activity-generally in response to elevated PI3K/Akt/mTOR signaling flux. There is thus much interest in exploring eIF4F as a small molecule target for the development of new anticancer drugs. The DEAD-box RNA helicase, eIF4A, is an essential subunit of eIF4F, and several potent small molecules (rocaglates, hippuristanol, pateamine A) affecting its activity have been identified and shown to demonstrate anticancer activity in vitro and in vivo in preclinical models. Recently, a number of new small molecules have been reported as having the capacity to target and inhibit eIF4A. Here, we undertook a comparative analysis of their biological activity and specificity relative to the eIF4A inhibitor, hippuristanol.

Original languageEnglish (US)
Pages (from-to)541-549
Number of pages9
Issue number5
StatePublished - May 2020
Externally publishedYes


  • EIF4A
  • EIF4F
  • Hippuristanol
  • RNA helicase
  • Translation initiation

ASJC Scopus subject areas

  • Molecular Biology


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