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Article Open Access

Anti‑breast cancer activity of selected 1,3,5‑triazines via modulation of EGFR‑TK

  • Authors:
    • Weixin Yan
    • Yiyang Zhao
    • Jianrong He
  • View Affiliations / Copyright

    Affiliations: State Key Lab of Mechanical System and Vibration, Robotics Institute, Shanghai Jiao Tong University, Shanghai 200240, P.R. China, Comprehensive Breast Health Center, Shanghai Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, P.R. China
    Copyright: © Yan et al. This is an open access article distributed under the terms of Creative Commons Attribution License.
  • Pages: 4175-4184
    |
    Published online on: August 24, 2018
       https://doi.org/10.3892/mmr.2018.9426
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Abstract

The present study investigated the effect of certain 1,3,5‑triazine derivatives on epidermal growth factor receptor‑tyrosine kinase (EGFR‑TK). The results suggested that 1,3,5‑triazine derivatives exhibited optimal drug likeness via molinspiration and proved to be effective drug candidates as potential anticancer agents. The molecules were demonstrated to interact with key catalytic residues of EGFR, including Asn818, Lys721, Leu694, Val702 and Met742 as demonstrated in molecular docking experiments. Compound 1d was demonstrated to be the most potent analogue with an inhibitory constant of 0.44 nM, against EGFR‑TK in in‑vitro enzyme inhibition assay. Compound 1d was further evaluated for its effect on the cellular viability of three breast cancer cell lines, including highly metastatic MDAMB231, human epidermal growth factor receptor 2‑positive BT474 and estrogen receptorpositive MCF7 cells, using an MTT assay and apoptosis analysis. Western blot analysis was performed to examine the levels of β‑catenin in the control and treated cells. Based on the findings of the current study, the chemical 1,3,5‑triazine series are potential novel inhibitors of EGFR‑TK and β‑catenin signaling, and may be potent anti‑breast cancer agents.
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Copy and paste a formatted citation
Spandidos Publications style
Yan W, Zhao Y and He J: Anti‑breast cancer activity of selected 1,3,5‑triazines via modulation of EGFR‑TK. Mol Med Rep 18: 4175-4184, 2018.
APA
Yan, W., Zhao, Y., & He, J. (2018). Anti‑breast cancer activity of selected 1,3,5‑triazines via modulation of EGFR‑TK. Molecular Medicine Reports, 18, 4175-4184. https://doi.org/10.3892/mmr.2018.9426
MLA
Yan, W., Zhao, Y., He, J."Anti‑breast cancer activity of selected 1,3,5‑triazines via modulation of EGFR‑TK". Molecular Medicine Reports 18.5 (2018): 4175-4184.
Chicago
Yan, W., Zhao, Y., He, J."Anti‑breast cancer activity of selected 1,3,5‑triazines via modulation of EGFR‑TK". Molecular Medicine Reports 18, no. 5 (2018): 4175-4184. https://doi.org/10.3892/mmr.2018.9426
Copy and paste a formatted citation
x
Spandidos Publications style
Yan W, Zhao Y and He J: Anti‑breast cancer activity of selected 1,3,5‑triazines via modulation of EGFR‑TK. Mol Med Rep 18: 4175-4184, 2018.
APA
Yan, W., Zhao, Y., & He, J. (2018). Anti‑breast cancer activity of selected 1,3,5‑triazines via modulation of EGFR‑TK. Molecular Medicine Reports, 18, 4175-4184. https://doi.org/10.3892/mmr.2018.9426
MLA
Yan, W., Zhao, Y., He, J."Anti‑breast cancer activity of selected 1,3,5‑triazines via modulation of EGFR‑TK". Molecular Medicine Reports 18.5 (2018): 4175-4184.
Chicago
Yan, W., Zhao, Y., He, J."Anti‑breast cancer activity of selected 1,3,5‑triazines via modulation of EGFR‑TK". Molecular Medicine Reports 18, no. 5 (2018): 4175-4184. https://doi.org/10.3892/mmr.2018.9426
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