Discovery of oxazine-linked pyrimidine as an inhibitor of breast cancer growth and metastasis by abrogating NF-κB activation Article Swipe
Jie Yuan
,
Bhanuprakash C. Narasimhachar
,
Akshay Ravish
,
Yang Li
,
Hua Zhang
,
Qun Wang
,
Zhi Li
,
Jun Huang
,
Bei Wang
,
Geng Wang
,
Keshav Kumar Harish
,
Arunachalam Chinnathambi
,
Chandramohan Govindasamy
,
M. Mahendra
,
Basappa Basappa
·
YOU?
·
· 2024
· Open Access
·
· DOI: https://doi.org/10.3389/fonc.2024.1390992
YOU?
·
· 2024
· Open Access
·
· DOI: https://doi.org/10.3389/fonc.2024.1390992
Introduction Nuclear factor kappa (NF-κB) plays a key role in cancer cell proliferation; thus, small molecule inhibitors of NF-κB activity can effectively inhibit breast cancer (BC) progression. We have previously reported oxazine and piperazine-linked pyrimidines as novel anti-cancer agents that can suppress NF-κB activation in BC cells. Moreover, the TRX-01 compound, an oxazine-linked pyrimidine, inhibited MCF-7 cells at a concentration of 9.17 µM in the Alamar Blue assay. Methods This work involved the analysis of frontier molecular orbitals, HOMO-LUMO interactions, and molecular electrostatic potential for the TRX-01 structure. Additionally, the TRX-01 compound was studied for cytotoxicity, and migration as well as invasion assays were performed on BC cells. Results Finally, TRX-01 blocked the translocation of NF-κB from the cytoplasm to the nucleus in MCF-7 cells and reduced NF-κB and IκBα levels in a dose-dependent manner. It also suppressed migratory and invasive properties of BC cells. Conclusion Overall, the data indicates that TRX-01 can function as a novel blocker of BC growth and metastasis by targeting NF-κB activation.
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Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.3389/fonc.2024.1390992
- https://www.frontiersin.org/journals/oncology/articles/10.3389/fonc.2024.1390992/pdf
- OA Status
- gold
- Cited By
- 4
- References
- 42
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W4401101310
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Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W4401101310Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.3389/fonc.2024.1390992Digital Object Identifier
- Title
-
Discovery of oxazine-linked pyrimidine as an inhibitor of breast cancer growth and metastasis by abrogating NF-κB activationWork title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
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2024Year of publication
- Publication date
-
2024-07-29Full publication date if available
- Authors
-
Jie Yuan, Bhanuprakash C. Narasimhachar, Akshay Ravish, Yang Li, Hua Zhang, Qun Wang, Zhi Li, Jun Huang, Bei Wang, Geng Wang, Keshav Kumar Harish, Arunachalam Chinnathambi, Chandramohan Govindasamy, M. Mahendra, Basappa BasappaList of authors in order
- Landing page
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https://doi.org/10.3389/fonc.2024.1390992Publisher landing page
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https://www.frontiersin.org/journals/oncology/articles/10.3389/fonc.2024.1390992/pdfDirect link to full text PDF
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YesWhether a free full text is available
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goldOpen access status per OpenAlex
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https://www.frontiersin.org/journals/oncology/articles/10.3389/fonc.2024.1390992/pdfDirect OA link when available
- Concepts
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Cancer research, Breast cancer, Metastasis, NF-κB, Cancer cell, Pyrimidine, Cancer, NFKB1, Chemistry, Cell growth, Small molecule, Medicine, Signal transduction, Transcription factor, Biochemistry, Internal medicine, GeneTop concepts (fields/topics) attached by OpenAlex
- Cited by
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4Total citation count in OpenAlex
- Citations by year (recent)
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2025: 4Per-year citation counts (last 5 years)
- References (count)
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42Number of works referenced by this work
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10Other works algorithmically related by OpenAlex
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