Discovery of epi-Enprioline as a Novel Drug for the Treatment of Vincristine Resistant Neuroblastoma
Neuroblastoma is a childhood solid tumour originating from undifferentiated neural progenitor cells of the sympathetic nervous system. Drug resistance of childhood cancer neuroblastoma is a serious clinical problem. In the present study, we aimed to identify novel drugs that can inhibit the growth and survival of chemoresistant neuroblastoma. High-throughput screening identified a small molecule, epi-enprioline that was able to induce apoptosis of vincristine-resistant neuroblastoma cells via the mitochondrial apoptotic pathway. Epi-enprioline reduced tumour growth in multiple preclinical models, including an orthotopic neuroblastoma patient-derived xenograft model in vivo. In summary, our data suggest that epi-enprioline can be considered as a lead compound for the treatment of vincristine-resistant neuroblastoma uncovering a novel strategy, which can be further explored as a treatment for drug-resistant neuroblastoma.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:21 |
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| Enthalten in: |
International journal of molecular sciences - 21(2020), 18 vom: 08. Sept. |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Sime, Wondossen [VerfasserIn] |
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| Links: |
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| Themen: |
5J49Q6B70F |
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| Anmerkungen: |
Date Completed 11.03.2021 Date Revised 11.03.2021 published: Electronic Citation Status MEDLINE |
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| doi: |
10.3390/ijms21186577 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM314840648 |
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| 520 | |a Neuroblastoma is a childhood solid tumour originating from undifferentiated neural progenitor cells of the sympathetic nervous system. Drug resistance of childhood cancer neuroblastoma is a serious clinical problem. In the present study, we aimed to identify novel drugs that can inhibit the growth and survival of chemoresistant neuroblastoma. High-throughput screening identified a small molecule, epi-enprioline that was able to induce apoptosis of vincristine-resistant neuroblastoma cells via the mitochondrial apoptotic pathway. Epi-enprioline reduced tumour growth in multiple preclinical models, including an orthotopic neuroblastoma patient-derived xenograft model in vivo. In summary, our data suggest that epi-enprioline can be considered as a lead compound for the treatment of vincristine-resistant neuroblastoma uncovering a novel strategy, which can be further explored as a treatment for drug-resistant neuroblastoma | ||
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| 700 | 1 | |a Abassi, Yasmin |e verfasserin |4 aut | |
| 700 | 1 | |a Lasorsa, Vito Alessandro |e verfasserin |4 aut | |
| 700 | 1 | |a Bonne Køhler, Julie |e verfasserin |4 aut | |
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| 700 | 1 | |a Strand, Daniel |e verfasserin |4 aut | |
| 700 | 1 | |a Capasso, Mario |e verfasserin |4 aut | |
| 700 | 1 | |a Massoumi, Ramin |e verfasserin |4 aut | |
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