BET inhibition as a new strategy for the treatment of gastric cancer Article Swipe
Raquel Carvalho Montenegro
,
Peter G. K. Clark
,
Alison Howarth
,
Xiao Wan
,
Alessandro Ceroni
,
Paulina Siejka
,
G. Nunez-Alonso
,
Octovia Monteiro
,
Catherine Rogers
,
Vicki Gamble
,
Rommel Mário Rodríguez Burbano
,
Paul E. Brennan
,
C. Tallant
,
Daniel Ebner
,
O. Fedorov
,
Eric O’Neill
,
Stefan Knapp
,
Darren J. Dixon
,
Susanne Müller
·
YOU?
·
· 2016
· Open Access
·
· DOI: https://doi.org/10.18632/oncotarget.9766
YOU?
·
· 2016
· Open Access
·
· DOI: https://doi.org/10.18632/oncotarget.9766
Gastric cancer is one of the most common malignancies and a leading cause of cancer death worldwide. The prognosis of stomach cancer is generally poor as this cancer is not very sensitive to commonly used chemotherapies. Epigenetic modifications play a key role in gastric cancer and contribute to the development and progression of this malignancy. In order to explore new treatment options in this target area we have screened a library of epigenetic inhibitors against gastric cancer cell lines and identified inhibitors for the BET family of bromodomains as potent inhibitors of gastric cancer cell proliferations. Here we show that both the pan-BET inhibitor (+)-JQ1 as well as a newly developed specific isoxazole inhibitor, PNZ5, showed potent inhibition of gastric cancer cell growth. Intriguingly, we found differences in the antiproliferative response between gastric cancer cells tested derived from Brazilian patients as compared to those from Asian patients, the latter being largely resistant to BET inhibition. As BET inhibitors are entering clinical trials these findings provide the first starting point for future therapies targeting gastric cancer.
Related Topics
Concepts
Cancer
Medicine
Bromodomain
Cancer research
Cancer cell
BET inhibitor
Epigenetics
Malignancy
Internal medicine
Biology
Biochemistry
Gene
Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.18632/oncotarget.9766
- OA Status
- diamond
- Cited By
- 52
- References
- 72
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W2412923902
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W2412923902Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.18632/oncotarget.9766Digital Object Identifier
- Title
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BET inhibition as a new strategy for the treatment of gastric cancerWork title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
-
2016Year of publication
- Publication date
-
2016-06-01Full publication date if available
- Authors
-
Raquel Carvalho Montenegro, Peter G. K. Clark, Alison Howarth, Xiao Wan, Alessandro Ceroni, Paulina Siejka, G. Nunez-Alonso, Octovia Monteiro, Catherine Rogers, Vicki Gamble, Rommel Mário Rodríguez Burbano, Paul E. Brennan, C. Tallant, Daniel Ebner, O. Fedorov, Eric O’Neill, Stefan Knapp, Darren J. Dixon, Susanne MüllerList of authors in order
- Landing page
-
https://doi.org/10.18632/oncotarget.9766Publisher landing page
- Open access
-
YesWhether a free full text is available
- OA status
-
diamondOpen access status per OpenAlex
- OA URL
-
https://doi.org/10.18632/oncotarget.9766Direct OA link when available
- Concepts
-
Cancer, Medicine, Bromodomain, Cancer research, Cancer cell, BET inhibitor, Epigenetics, Malignancy, Internal medicine, Biology, Biochemistry, GeneTop concepts (fields/topics) attached by OpenAlex
- Cited by
-
52Total citation count in OpenAlex
- Citations by year (recent)
-
2025: 4, 2024: 3, 2023: 5, 2022: 6, 2021: 3Per-year citation counts (last 5 years)
- References (count)
-
72Number of works referenced by this work
- Related works (count)
-
10Other works algorithmically related by OpenAlex
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| abstract_inverted_index.target | 64 |
| abstract_inverted_index.tested | 135 |
| abstract_inverted_index.trials | 161 |
| abstract_inverted_index.(+)-JQ1 | 104 |
| abstract_inverted_index.Gastric | 0 |
| abstract_inverted_index.against | 74 |
| abstract_inverted_index.between | 131 |
| abstract_inverted_index.cancer. | 174 |
| abstract_inverted_index.derived | 136 |
| abstract_inverted_index.explore | 58 |
| abstract_inverted_index.gastric | 43, 75, 92, 119, 132, 173 |
| abstract_inverted_index.growth. | 122 |
| abstract_inverted_index.largely | 150 |
| abstract_inverted_index.leading | 11 |
| abstract_inverted_index.library | 70 |
| abstract_inverted_index.options | 61 |
| abstract_inverted_index.pan-BET | 102 |
| abstract_inverted_index.provide | 164 |
| abstract_inverted_index.stomach | 20 |
| abstract_inverted_index.clinical | 160 |
| abstract_inverted_index.commonly | 33 |
| abstract_inverted_index.compared | 141 |
| abstract_inverted_index.entering | 159 |
| abstract_inverted_index.findings | 163 |
| abstract_inverted_index.patients | 139 |
| abstract_inverted_index.response | 130 |
| abstract_inverted_index.screened | 68 |
| abstract_inverted_index.specific | 111 |
| abstract_inverted_index.starting | 167 |
| abstract_inverted_index.Brazilian | 138 |
| abstract_inverted_index.developed | 110 |
| abstract_inverted_index.generally | 23 |
| abstract_inverted_index.inhibitor | 103 |
| abstract_inverted_index.isoxazole | 112 |
| abstract_inverted_index.patients, | 146 |
| abstract_inverted_index.prognosis | 18 |
| abstract_inverted_index.resistant | 151 |
| abstract_inverted_index.sensitive | 31 |
| abstract_inverted_index.targeting | 172 |
| abstract_inverted_index.therapies | 171 |
| abstract_inverted_index.treatment | 60 |
| abstract_inverted_index.Epigenetic | 36 |
| abstract_inverted_index.contribute | 46 |
| abstract_inverted_index.epigenetic | 72 |
| abstract_inverted_index.identified | 80 |
| abstract_inverted_index.inhibition | 117 |
| abstract_inverted_index.inhibitor, | 113 |
| abstract_inverted_index.inhibitors | 73, 81, 90, 157 |
| abstract_inverted_index.worldwide. | 16 |
| abstract_inverted_index.development | 49 |
| abstract_inverted_index.differences | 126 |
| abstract_inverted_index.inhibition. | 154 |
| abstract_inverted_index.malignancy. | 54 |
| abstract_inverted_index.progression | 51 |
| abstract_inverted_index.bromodomains | 87 |
| abstract_inverted_index.malignancies | 8 |
| abstract_inverted_index.Intriguingly, | 123 |
| abstract_inverted_index.modifications | 37 |
| abstract_inverted_index.chemotherapies. | 35 |
| abstract_inverted_index.proliferations. | 95 |
| abstract_inverted_index.antiproliferative | 129 |
| cited_by_percentile_year.max | 99 |
| cited_by_percentile_year.min | 95 |
| countries_distinct_count | 2 |
| institutions_distinct_count | 19 |
| sustainable_development_goals[0].id | https://metadata.un.org/sdg/3 |
| sustainable_development_goals[0].score | 0.7799999713897705 |
| sustainable_development_goals[0].display_name | Good health and well-being |
| citation_normalized_percentile.value | 0.9499107 |
| citation_normalized_percentile.is_in_top_1_percent | False |
| citation_normalized_percentile.is_in_top_10_percent | True |