Evidence map›Paper›PMID 24946763›Full record

ArticleOncotarget2014

HER2-signaling pathway, JNK and ERKs kinases, and cancer stem-like cells are targets of Bozepinib small compound.

Alberto Ramírez, Houria Boulaiz, Cynthia Morata-Tarifa, Macarena Perán, Gema Jiménez, Manuel Picon-Ruiz, Ahmad Agil, Olga Cruz-López, Ana Conejo-García, Joaquín M Campos and 3 more

Open access · diamondAbstract read
In one paragraph

Article in Oncotarget, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
2.7field-weighted citation impact, top 11% 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

14 citing papers in PubMed, 29 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Article
  6. Article
  7. Article
  8. Article
  9. GLI1: A Therapeutic Target for Cancer.Frontiers in oncology · 2021
    Review
  10. Article
  11. Enhancement of Tumor Cell Death by CombiningFrontiers in pharmacology · 2018
    Article
  12. Article
  13. Review
  14. 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

13 authors at 6 institutions in 2 countries.

Alberto RamírezDepartment of Health Sciences, University of Jaén, Jaén, Spain.
Houria Boulaiz
Cynthia Morata-Tarifa
Macarena Perán
Gema Jiménez
Manuel Picon-Ruiz
Ahmad Agil
Olga Cruz-López
Ana Conejo-García
Joaquín M Campos
Ana Sánchez
María A GarcíaBiopathology and Medicine Regenerative Institute (IBIMER), University of Granada, Granada, Spain; Biosanitary Institute of Granada (ibs.GRANADA), SAS-Universidad de Granada, Granada, Spain; Department of Oncology, Virgen de las Nieves, University Hospital, Granada, Spain.
Juan A MarchalDepartment of Human Anatomy and Embryology, University of Granada, Granada, Spain; Biopathology and Medicine Regenerative Institute (IBIMER), University of Granada, Granada, Spain; Biosanitary Institute of Granada (ibs.GRANADA), SAS-Universidad de Granada, Granada, Spain.
Instituto de Investigación Biosanitaria de Granada · ESComplejo Hospitalario Universitario de Granada · ESUniversidad de Granada · ESUniversidad de Jaén · ESAndalusian School of Public Health · ESUniversity of Miami · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Identification of novel anticancer drugs presenting more than one molecular target and efficacy against cancer stem-like cells (CSCs) subpopulations represents a therapeutic need to combat the resistance and the high risk of relapse in patients. In the present work we show how Bozepinib [(RS)-2,6-dichloro-9-[1-(p-nitrobenzenesulfonyl)-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]-9H-purine], a small anti-tumor compound, demonstrated selectivity on cancer cells and showed an inhibitory effect over kinases involved in carcinogenesis, proliferation and angiogenesis. The cytotoxic effects of Bozepinib were observed in both breast and colon cancer cells expressing different receptor patterns. Bozepinib inhibited HER-2 signaling pathway and JNK and ERKs kinases. In addition, Bozepinib has an inhibitory effect on AKT and VEGF together with anti-angiogenic and anti-migratory activities. Moreover, the modulation of pathways involved in tumorigenesis by Bozepinib was also evident in microarrays analysis. Interestingly, Bozepinib inhibited both mamo- and colono-spheres formation and eliminated ALDH+ CSCs subpopulations at a low micromolar range similar to Salinomycin. Bozepinib induced the down-regulation of c-MYC, β-CATENIN and SOX2 proteins and the up-regulation of the GLI-3 hedgehog-signaling repressor. Finally, Bozepinib shows in vivo anti-tumor and anti-metastatic efficacy in xenotransplanted nude mice without presenting sub-acute toxicity. These findings support further studies on the therapeutic potential of Bozepinib in cancer patients.

Indexed as

AnimalsBreast NeoplasmsCaco-2 CellsCell Line, TumorColonic NeoplasmsErb-b2 Receptor Tyrosine KinasesExtracellular Signal-Regulated MAP KinasesFemaleHCT116 CellsHT29 CellsHumansJNK Mitogen-Activated Protein KinasesMCF-7 CellsMiceMice, Inbred BALB CNeoplasm Metastasis2,6-dichloro-9-(1-(p-nitrobenzenesulfonyl)-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl)-9H-purineERBB2 protein, humanErb-b2 Receptor Tyrosine KinasesExtracellular Signal-Regulated MAP KinasesJNK Mitogen-Activated Protein KinasesOxazepinesPurines

Identifiers

PMID24946763
PMCPMC4116505
OpenAlexW1899392978

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.