ArticleEuropean journal of pharmacology2017
A harmine-derived beta-carboline displays anti-cancer effects in vitro by targeting protein synthesis.
Article in European journal of pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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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.
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Who cites it
24 citing papers in PubMed, 57 citations in OpenAlex.
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- The Revolution of Targeted Therapies in Thyroid Cancer Treatment: Present and Future Promising Anti-Cancer Drugs.International journal of molecular sciences · 2025Review
- Exploiting Translation Machinery for Cancer Therapy: Translation Factors as Promising Targets.International journal of molecular sciences · 2024Review
- Protein translation: biological processes and therapeutic strategies for human diseases.Signal transduction and targeted therapy · 2024Review
- Research progress on the antitumor effects of harmine.Frontiers in oncology · 2024Review
- Intricate subcellular journey of nanoparticles to the enigmatic domains of endoplasmic reticulum.Drug delivery · 2023Review
- Anthranilamides with quinoline and β-carboline scaffolds: design, synthesis, and biological activity.Molecular diversity · 2022Article
- Harmine is an effective therapeutic small molecule for the treatment of cardiac hypertrophy.Acta pharmacologica Sinica · 2022Article
- Synthetic Biology in Plants, a Boon for Coming Decades.Molecular biotechnology · 2021Review
- Bioactive antifungal metabolites produced by Streptomyces amritsarensis V31 help to control diverse phytopathogenic fungi.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2021Article
- Design and Synthesis of Fluorescent 1,3-Diaryl-β-carbolines and 1,3-Diaryl-3,4-dihydro-β-carbolines.ACS omega · 2021Article
- Antimicrobial Activity of a Repurposed Harmine-Derived Compound on Carbapenem-ResistantFrontiers in cellular and infection microbiology · 2021Article
- A Quick Guide to Small-Molecule Inhibitors of Eukaryotic Protein Synthesis.Biochemistry. Biokhimiia · 2020Review
- Recent evolution on synthesis strategies and anti-leishmanial activity of β-carboline derivatives - An update.Heliyon · 2020Review
- Eukaryotic translation initiation factor 3 subunit b is a novel oncogenic factor in prostate cancer.Mammalian genome : official journal of the International Mammalian Genome Society · 2020Article
- Identification and Repurposing of Trisubstituted Harmine Derivatives as Novel Inhibitors ofMolecules (Basel, Switzerland) · 2020Article
- Novel Hybrid CHC from β-carboline andFrontiers in pharmacology · 2020Article
- Design and Synthesis of a New Soluble Natural β-Carboline Derivative for Preclinical Study by Intravenous Injection.International journal of molecular sciences · 2019Article
- Harmine suppresses hyper-activated Ras-MAPK pathway by selectively targeting oncogenic mutated Ras/Raf inCancer cell international · 2019Article
- BCESA: a nano-scaled intercalator capable of targeting tumor tissue and releasing anti-tumoral β-carboline-3-carboxylic acid.International journal of nanomedicine · 2019Article
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 3 countries.
Funding
Abstract
Growing evidence indicates that protein synthesis is deregulated in cancer onset and progression and targeting this process might be a selective way to combat cancers. While harmine is known to inhibit DYRK1A and intercalate into the DNA, tri-substitution was shown previously to modify its activity profile in favor of protein synthesis inhibition. In this study, we thus evaluated the optimized derivative CM16 in vitro anti-cancer effects unfolding its protein synthesis inhibition activity. Indeed, the growth inhibitory profile of CM16 in the NCI 60-cancer-cell-line-panel correlated with those of other compounds described as protein synthesis inhibitors. Accordingly, CM16 decreased in a time- and concentration-dependent manner the translation of neosynthesized proteins in vitro while it did not affect mRNA transcription. CM16 rapidly penetrated into the cell in the perinuclear region of the endoplasmic reticulum where it appears to target translation initiation as highlighted by ribosomal disorganization. More precisely, we found that the mRNA expression levels of the initiation factors EIF1AX, EIF3E and EIF3H differ when comparing resistant or sensitive cell models to CM16. Additionally, CM16 induced eIF2α phosphorylation. Those effects could explain, at least partly, the CM16 cytostatic anti-cancer effects observed in vitro while neither cell cycle arrest nor DNA intercalation could be demonstrated. Therefore, targeting protein synthesis initiation with CM16 could represent a new promising alternative to current cancer therapies due to the specific alterations of the translation machinery in cancer cells as recently evidenced with respect to EIF1AX and eIF3 complex, the potential targets identified in this present study.
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