Inhibition of epidermal growth factor receptor by ferulic acid and 4-vinylguaiacol in human breast cancer cells
Inhibition of epidermal growth factor receptor by ferulic acid and 4-vinylguaiacol in human breast cancer cells
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DOI：
10.1007/s10529-017-2475-2
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发表时间：
2018-02-01
影响因子：
2.7
通讯作者：
Lakshmi, B. S.
中科院分区：
文献类型：
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作者：
Sudhagar, S.;Sathya, S.;Lakshmi, B. S.
目的 研究阿魏酸和 4-乙烯基愈创木酚在体外抑制人乳腺癌细胞表皮生长因子受体 (EGFR) 的潜力。阿魏酸和 4-乙烯基愈创木酚限制 EGF（表皮生长因子）诱导的乳腺癌增殖和新 DNA 合成。蛋白质印迹分析显示阿魏酸和 4-乙烯基愈创木酚通过下调 Tyr 1068 自磷酸化表现出对 EGFR 激活的持续抑制。分子对接分析显示阿魏酸与Lys 745和Met 793形成氢键相互作用，而4-乙烯基愈创木酚与Phe 856形成两个氢键，并与EGFR激酶结构域的多个氨基酸残基表现出更强的疏水相互作用。阿魏酸和4-乙烯基愈创木酚可以作为开发针对EGFR的新型小分子疗法的潜在结构。
To examine the potential of ferulic acid and 4-vinylguaiacol for inhibiting epidermal growth factor receptor (EGFR) in human breast cancer cells in vitro.Ferulic acid and 4-vinylguaiacol limit the EGF (epidermal growth factor)-induced breast cancer proliferation and new DNA synthesis. Western blot analysis revealed both ferulic acid and 4-vinylguaiacol exhibit sustained inhibition of EGFR activation through down-regulation of Tyr 1068 autophosphorylation. Molecular docking analysis shows ferulic acid forming hydrogen bond interaction with Lys 745 and Met 793 whereas, 4-vinylguaiacol forms two hydrogen bonds with Phe 856 and exhibits stronger hydrophobic interactions with multiple amino acid residues at the EGFR kinase domain.Ferulic acid and 4-vinylguaiacol could serve as a potential structure for the development of new small molecule therapeutics against EGFR.