ArticlePloS one2015
A Novel Time-Dependent CENP-E Inhibitor with Potent Antitumor Activity.
Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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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.
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.
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Who cites it
20 citing papers in PubMed, 34 citations in OpenAlex.
- CENPW knockdown inhibits progression of bladder cancer through inducing cell cycle arrest and apoptosis.Journal of Cancer · 2024Article
- Kinesin-7 CENP-E in tumorigenesis: Chromosome instability, spindle assembly checkpoint, and applications.Frontiers in molecular biosciences · 2024Review
- RZZ-Spindly and CENP-E form an integrated platform to recruit dynein to the kinetochore corona.The EMBO journal · 2023Article
- CENP-E activation by Aurora A and B controls kinetochore fibrous corona disassembly.Nature communications · 2023Article
- Tetraploidy-linked sensitization to CENP-E inhibition in human cells.Molecular oncology · 2023Article
- A mechanism that integrates microtubule motors of opposite polarity at the kinetochore corona.bioRxiv : the preprint server for biology · 2023Article
- Post-translational modifications of tubulin: their role in cancers and the regulation of signaling molecules.Cancer gene therapy · 2023Review
- Second-Generation Antimitotics in Cancer Clinical Trials.Pharmaceutics · 2021Review
- A CDC7 inhibitor sensitizes DNA-damaging chemotherapies by suppressing homologous recombination repair to delay DNA damage recovery.Science advances · 2021Article
- Mitotic Poisons in Research and Medicine.Molecules (Basel, Switzerland) · 2020Review
- Distinct Mechanisms of Resistance to a CENP-E Inhibitor Emerge in Near-Haploid and Diploid Cancer Cells.Cell chemical biology · 2020Article
- Review
- Molecular mechanism and potential target indication of TAK-931, a novel CDC7-selective inhibitor.Science advances · 2019Article
- GSK923295 as a potential antihepatocellular carcinoma agent causing delay on liver regeneration after partial hepatectomy.Chinese medical journal · 2019Article
- Proliferation of aneuploid cells induced by CENP-E depletion is counteracted by the p14Molecular genetics and genomics : MGG · 2019Article
- Natural products as new antimitotic compounds for anticancer drug development.Clinics (Sao Paulo, Brazil) · 2018Review
- Mechanisms of Chromosome Congression during Mitosis.Biology · 2017Review
- Motor activity of centromere-associated protein-E contributes to its localization at the center of the midbody to regulate cytokinetic abscission.Oncotarget · 2016Article
- α-Fodrin-CENP-E interaction is critical for pancreatic cancer progression and drug response.Cell cycle (Georgetown, Tex.)Article
- Leveraging Kinesin Family as Key Regulators of Malignant Progression and the Immunometabolic Niche for Precision Oncology.Technology in cancer research & treatmentReview
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Centromere-associated protein E (CENP-E) regulates both chromosome congression and the spindle assembly checkpoint (SAC) during mitosis. The loss of CENP-E function causes chromosome misalignment, leading to SAC activation and apoptosis during prolonged mitotic arrest. Here, we describe the biological and antiproliferative activities of a novel small-molecule inhibitor of CENP-E, Compound-A (Cmpd-A). Cmpd-A inhibits the ATPase activity of the CENP-E motor domain, acting as a time-dependent inhibitor with an ATP-competitive-like behavior. Cmpd-A causes chromosome misalignment on the metaphase plate, leading to prolonged mitotic arrest. Treatment with Cmpd-A induces antiproliferation in multiple cancer cell lines. Furthermore, Cmpd-A exhibits antitumor activity in a nude mouse xenograft model, and this antitumor activity is accompanied by the elevation of phosphohistone H3 levels in tumors. These findings demonstrate the potency of the CENP-E inhibitor Cmpd-A and its potential as an anticancer therapeutic agent.
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Registered trials
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.