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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...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
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.
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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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