Evidence map›Paper›PMID 31519508›Full record

ArticleCell chemical biology2019

Amidino-Rocaglates: A Potent Class of eIF4A Inhibitors.

Jennifer Chu, Wenhan Zhang, Regina Cencic, William G Devine, Dmitri Beglov, Thomas Henkel, Lauren E Brown, Sandor Vajda, John A Porco, Jerry Pelletier

Open access · bronzeAbstract read
In one paragraph

Article in Cell chemical biology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.

0numbers the graph read from it
0cells of the map it votes in
59citing papers in PubMed
2.9field-weighted citation impact, top 8% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

59 citing papers in PubMed, 76 citations in OpenAlex.

  1. Review
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  10. eIF4A controls translation of estrogen receptor alpha and is a therapeutic target in advanced breast cancer.Proceedings of the National Academy of Sciences of the United States of America · 2025
    Article
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  18. Pharmacologic Inhibition of EIF4A Blocks NRF2 Synthesis to Prevent Osteosarcoma Metastasis.Clinical cancer research : an official journal of the American Association for Cancer Research · 2024
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 2 institutions in 2 countries.

Jennifer ChuDepartment of Biochemistry, McGill University, Montreal, QC H3G 1Y6, Canada.
Wenhan ZhangDepartment of Chemistry, 590 Commonwealth Avenue, Boston University, Boston, MA 02215, USA; Center for Molecular Discovery (BU-CMD), Boston University, Boston, MA, USA.
Regina CencicDepartment of Biochemistry, McGill University, Montreal, QC H3G 1Y6, Canada.
William G DevineDepartment of Chemistry, 590 Commonwealth Avenue, Boston University, Boston, MA 02215, USA; Center for Molecular Discovery (BU-CMD), Boston University, Boston, MA, USA.
Dmitri BeglovDepartment of Biomedical Engineering, Boston University, Boston, MA, USA.
Thomas HenkelIMAX Discovery GmbH, Dortmund, Germany.
Lauren E BrownDepartment of Chemistry, 590 Commonwealth Avenue, Boston University, Boston, MA 02215, USA; Center for Molecular Discovery (BU-CMD), Boston University, Boston, MA, USA.
Sandor VajdaDepartment of Chemistry, 590 Commonwealth Avenue, Boston University, Boston, MA 02215, USA; Department of Biomedical Engineering, Boston University, Boston, MA, USA.
John A PorcoDepartment of Chemistry, 590 Commonwealth Avenue, Boston University, Boston, MA 02215, USA; Center for Molecular Discovery (BU-CMD), Boston University, Boston, MA, USA. Electronic address: porco@bu.edu.
Jerry PelletierDepartment of Biochemistry, McGill University, Montreal, QC H3G 1Y6, Canada; Department of Oncology, McGill University, Montreal, Canada; Rosalind & Morris Goodman Cancer Research Centre, McGill University, Montreal, Canada. Electronic address: jerry.pelletier@mcgill.ca.
Boston University · USMcGill University · CA

Funding

SYNTHESIS OF LIBRARIES--LINEAR/POLYKETIDE/POLYPROPIONATEP50GM067041 · NIGMS · BOSTON UNIVERSITY MEDICAL CAMPUS · PI PORCO, JOHN A. · 2002 to 2012
$23.7M
Chemical Synthesis of Complex Natural Products for Translational ScienceR35GM118173 · NIGMS · BOSTON UNIVERSITY (CHARLES RIVER CAMPUS) · PI JOHN A. PORCO · 2016 to 2026
$8.2M
Analysis and Prediction of Molecular InteractionsR35GM118078 · NIGMS · BOSTON UNIVERSITY (CHARLES RIVER CAMPUS) · PI SANDOR VAJDA · 2016 to 2026
$6.5M
Center for Molecular Discovery (CMD): A Small Molecule Resource for Biomedical ResearchR24GM111625 · NIGMS · BOSTON UNIVERSITY (CHARLES RIVER CAMPUS) · PI PORCO, JOHN A. · 2015 to 2017
$1.5M
Canadian Institutes of Health Research FoundationNIGMS NIH HHS P50 GM067041NIGMS NIH HHS R24 GM111625NIGMS NIH HHS R35 GM118078NIGMS NIH HHS R35 GM118173
6 · The paper itself

Abstract

Rocaglates share a common cyclopenta[b]benzofuran core that inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase, eIF4A. Working as interfacial inhibitors, rocaglates stabilize the association between eIF4A and RNA, which can lead to the formation of steric barriers that block initiating ribosomes. There is significant interest in the development and expansion of rocaglate derivatives, as several members of this family have been shown to possess potent anti-neoplastic activity in vitro and in vivo. To further our understanding of rocaglate diversity and drug design, herein we explore the RNA clamping activity of >200 unique rocaglate derivatives. Through this, we report on the identification and characterization of a potent class of synthetic rocaglates called amidino-rocaglates. These compounds are among the most potent rocaglates documented to date and, taken together, this work offers important information that will guide the future design of rocaglates with improved biological properties.

Indexed as

AmidinesAnimalsAntineoplastic AgentsBenzofuransCell SurvivalDEAD-box RNA HelicasesDrug DesignEukaryotic Initiation Factor-4AFemaleHumansLymphomaMiceMice, Inbred C57BLProtein BiosynthesisRecombinant ProteinsRibosomesAmidinesAntineoplastic AgentsBenzofuransDEAD-box RNA HelicasesEIF4A2 protein, humanEukaryotic Initiation Factor-4ARecombinant ProteinsRNArocagloic acidamidino-rocaglateseIF4AeIF4Finterfacial inhibitortranslation initiation

Identifiers

PMID31519508
PMCPMC6874763
OpenAlexW2973112770

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.