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Targeting Dopamine Receptor D2 by Imipridone Suppresses Uterine Serous Cancer Malignant Phenotype
Uterine serous cancer (USC) is an aggressive subtype of endometrial cancer, with poor survival and high recurrence rates. The development of novel and effective therapies specific to USC would aid in its management. However, few studies have focused solely on this rare subtype. The current study dem...
Autores principales: | , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7563948/ https://www.ncbi.nlm.nih.gov/pubmed/32867127 http://dx.doi.org/10.3390/cancers12092436 |
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author | Hu, Wen Zhang, Li Ferri-Borgogno, Sammy Kwan, Suet-Ying Lewis, Kelsey E. Cun, Han T. Yeung, Tsz-Lun Soliman, Pamela T. Tarapore, Rohinton S. Allen, Joshua E. Guan, Xinyuan Lu, Karen H. Mok, Samuel C. Au-Yeung, Chi-Lam |
author_facet | Hu, Wen Zhang, Li Ferri-Borgogno, Sammy Kwan, Suet-Ying Lewis, Kelsey E. Cun, Han T. Yeung, Tsz-Lun Soliman, Pamela T. Tarapore, Rohinton S. Allen, Joshua E. Guan, Xinyuan Lu, Karen H. Mok, Samuel C. Au-Yeung, Chi-Lam |
author_sort | Hu, Wen |
collection | PubMed |
description | Uterine serous cancer (USC) is an aggressive subtype of endometrial cancer, with poor survival and high recurrence rates. The development of novel and effective therapies specific to USC would aid in its management. However, few studies have focused solely on this rare subtype. The current study demonstrated that the orally bioavailable, investigational new drug and novel imipridone ONC206 suppressed USC cell proliferation and induced apoptosis both in vitro and in vivo. Disruption of the DRD2-mediated p38MAPK/ERK/PGC-1α network by ONC206 led to metabolic reprogramming and suppression of both glycolysis and oxidative phosphorylation. ONC206 also synergized with paclitaxel in reducing USC cell viability. In addition, DRD2 overexpression correlated with poor overall survival in patients. This study provides the first evidence that ONC206 induced metabolic reprogramming in USC cells and is a promising therapeutic agent for USC treatment. These findings support further development of ONC206 as a promising therapeutic agent and improves survival rates in patients with USC. |
format | Online Article Text |
id | pubmed-7563948 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-75639482020-10-27 Targeting Dopamine Receptor D2 by Imipridone Suppresses Uterine Serous Cancer Malignant Phenotype Hu, Wen Zhang, Li Ferri-Borgogno, Sammy Kwan, Suet-Ying Lewis, Kelsey E. Cun, Han T. Yeung, Tsz-Lun Soliman, Pamela T. Tarapore, Rohinton S. Allen, Joshua E. Guan, Xinyuan Lu, Karen H. Mok, Samuel C. Au-Yeung, Chi-Lam Cancers (Basel) Article Uterine serous cancer (USC) is an aggressive subtype of endometrial cancer, with poor survival and high recurrence rates. The development of novel and effective therapies specific to USC would aid in its management. However, few studies have focused solely on this rare subtype. The current study demonstrated that the orally bioavailable, investigational new drug and novel imipridone ONC206 suppressed USC cell proliferation and induced apoptosis both in vitro and in vivo. Disruption of the DRD2-mediated p38MAPK/ERK/PGC-1α network by ONC206 led to metabolic reprogramming and suppression of both glycolysis and oxidative phosphorylation. ONC206 also synergized with paclitaxel in reducing USC cell viability. In addition, DRD2 overexpression correlated with poor overall survival in patients. This study provides the first evidence that ONC206 induced metabolic reprogramming in USC cells and is a promising therapeutic agent for USC treatment. These findings support further development of ONC206 as a promising therapeutic agent and improves survival rates in patients with USC. MDPI 2020-08-27 /pmc/articles/PMC7563948/ /pubmed/32867127 http://dx.doi.org/10.3390/cancers12092436 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Hu, Wen Zhang, Li Ferri-Borgogno, Sammy Kwan, Suet-Ying Lewis, Kelsey E. Cun, Han T. Yeung, Tsz-Lun Soliman, Pamela T. Tarapore, Rohinton S. Allen, Joshua E. Guan, Xinyuan Lu, Karen H. Mok, Samuel C. Au-Yeung, Chi-Lam Targeting Dopamine Receptor D2 by Imipridone Suppresses Uterine Serous Cancer Malignant Phenotype |
title | Targeting Dopamine Receptor D2 by Imipridone Suppresses Uterine Serous Cancer Malignant Phenotype |
title_full | Targeting Dopamine Receptor D2 by Imipridone Suppresses Uterine Serous Cancer Malignant Phenotype |
title_fullStr | Targeting Dopamine Receptor D2 by Imipridone Suppresses Uterine Serous Cancer Malignant Phenotype |
title_full_unstemmed | Targeting Dopamine Receptor D2 by Imipridone Suppresses Uterine Serous Cancer Malignant Phenotype |
title_short | Targeting Dopamine Receptor D2 by Imipridone Suppresses Uterine Serous Cancer Malignant Phenotype |
title_sort | targeting dopamine receptor d2 by imipridone suppresses uterine serous cancer malignant phenotype |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7563948/ https://www.ncbi.nlm.nih.gov/pubmed/32867127 http://dx.doi.org/10.3390/cancers12092436 |
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