Evidence map›Paper›PMID 36001933›Full record

ArticleEuropean journal of medicinal chemistry2022

Synthesis and biological evaluation of novel FiVe1 derivatives as potent and selective agents for the treatment of mesenchymal cancers.

Francisco Martínez-Peña, Aaron D Pearson, Eileen L Tang, Nick A Kuburich, Sendurai A Mani, Peter G Schultz, Michael J Bollong, Luke L Lairson

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
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

2 citing papers in PubMed.

  1. Review
  2. Article
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

8 authors.

Francisco Martínez-PeñaDepartment of Chemistry, The Scripps Research Institute, La Jolla, CA, 92037, USA.
Aaron D PearsonDepartment of Chemistry, The Scripps Research Institute, La Jolla, CA, 92037, USA.
Eileen L TangDepartment of Chemistry, The Scripps Research Institute, La Jolla, CA, 92037, USA.
Nick A KuburichDepartment of Translational Molecular Pathology, The University of Texas, MD, Anderson, USA.
Sendurai A ManiDepartment of Translational Molecular Pathology, The University of Texas, MD, Anderson, USA.
Peter G SchultzDepartment of Chemistry, The Scripps Research Institute, La Jolla, CA, 92037, USA.
Michael J BollongDepartment of Chemistry, The Scripps Research Institute, La Jolla, CA, 92037, USA. Electronic address: mbollong@scripps.edu.
Luke L LairsonDepartment of Chemistry, The Scripps Research Institute, La Jolla, CA, 92037, USA. Electronic address: llairson@scripps.edu.

Funding

Preclinical characterization of EMT/CSC-specific small molecule inhibitors for TNBCsR01CA200970 · NCI · UNIVERSITY OF TX MD ANDERSON CAN CTR · PI LAIRSON, LUKE LEE, MANI, SENDURAI AYYAVOO · 2017 to 2021
$2.7M
NCI NIH HHS R01 CA200970
6 · The paper itself

Abstract

Epithelial-mesenchymal transition (EMT) endows stem cell-like properties to cancer cells. Targeting this process represents a potential therapeutic approach to overcome cancer metastasis and chemotherapy resistance. FiVe1 was identified from an EMT-based synthetic lethality screen and was found to inhibit the stem cell-like properties and proliferation of not only cancer cells undergoing EMT, but also more broadly in mesenchymal cancers that include therapeutically intractable soft tissue sarcomas. FiVe1 functions by directly binding to the type III intermediate filament protein vimentin (VIM) in a mode that induces hyperphosphorylation of Ser56, which results in selective disruption of mitosis and induced multinucleation in transformed VIM-expressing mesenchymal cancer cell types. Cell-based potency (IC

Indexed as

Epithelial-Mesenchymal TransitionSarcomaAnimalsCell Line, TumorMiceMitosisPhosphorylationVimentinVimentinMedicinal chemistryMesenchymal cancerStructure-activity relationshipVimentin

Identifiers

PMID36001933
PMCPMC10377566

What OpenQuestion holds

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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.