ArticlePloS one2017
Selective small-chemical inhibitors of protein arginine methyltransferase 5 with anti-lung cancer activity.
Article in PloS one, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 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
11 citing papers in PubMed, 26 citations in OpenAlex.
- Decreased PPM1B Expression Drives PRMT5-Mediated Histone Modification in Lung Cancer Progression.Biomolecules · 2025Article
- Purification and Identification of Natural Inhibitors of Protein Arginine Methyltransferases from Plants.Molecular and cellular biology · 2022Article
- Acquired resistance to PRMT5 inhibition induces concomitant collateral sensitivity to paclitaxel.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- PRMT5 Selective Inhibitor Enhances Therapeutic Efficacy of Cisplatin in Lung Cancer Cells.International journal of molecular sciences · 2021Article
- Biology of the mRNA Splicing Machinery and Its Dysregulation in Cancer Providing Therapeutic Opportunities.International journal of molecular sciences · 2021Review
- A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6.Journal of medicinal chemistry · 2021Article
- WD Repeat Domain 77 Protein Regulates Translation of E2F1 and E2F3 mRNA.Molecular and cellular biology · 2020Article
- Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders.Journal of medicinal chemistry · 2020Article
- Rational Design, synthesis and biological evaluation of novel triazole derivatives as potent and selective PRMT5 inhibitors with antitumor activity.Journal of computer-aided molecular design · 2019Article
- Curcumin ameliorates PRMT5-MEP50 arginine methyltransferase expression by decreasing the Sp1 and NF-YA transcription factors in the A549 and MCF-7 cells.Molecular and cellular biochemistry · 2019Article
- The methylation induced by protein arginine methyltransferase 5 promotes tumorigenesis and progression of lung cancer.Journal of thoracic disease · 2018Review
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 5 institutions in 2 countries.
Funding
Abstract
Protein arginine methyltransferase 5 (PRMT5) plays critical roles in a wide variety of biological processes, including tumorigenesis. By screening a library of small chemical compounds, we identified eight compounds that selectively inhibit the PRMT5 enzymatic activity, with IC50 values ranging from 0.1 to 6 μM. Molecular docking simulation and site-directed mutagenesis indicated that identified compounds target the substrate-binding site in PRMT5. Treatment of lung cancer cells with identified inhibitors led to inhibition of the symmetrical arginine methylation of SmD3 and histones and the cellular proliferation. Oral administration of the inhibitor demonstrated antitumor activity in a lung tumor xenograft model. Thus, identified PRMT5-specific small-molecule inhibitors would help elucidate the biological roles of PRMT5 and serve as lead compounds for future drug development.
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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.