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.
journal_name
Mol Med Repjournal_title
Molecular medicine reportsauthors
Yan W,Zhao Y,He Jdoi
10.3892/mmr.2018.9426subject
Has Abstractpub_date
2018-11-01 00:00:00pages
4175-4184issue
5eissn
1791-2997issn
1791-3004journal_volume
18pub_type
杂志文章abstract::The tumor suppressor protein LKB1 is a serine/threonine kinase that plays a critical role in cell proliferation, and its inactivation has been linked to tumorigenesis in various cancer types. Current understanding of the LKB1 function is largely restricted to results from experiments on LKB1‑deficient cancer cells, wh...
journal_title:Molecular medicine reports
pub_type: 杂志文章
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pub_type: 杂志文章,评审
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journal_title:Molecular medicine reports
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pub_type: 杂志文章
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pub_type: 杂志文章
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pub_type: 杂志文章
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pub_type: 临床试验,杂志文章,多中心研究
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