Journal
BIOTECHNOLOGY LETTERS
Volume 40, Issue 2, Pages 257-262Publisher
SPRINGER
DOI: 10.1007/s10529-017-2475-2
Keywords
Breast cancer; Epidermal growth factor receptor; Ferulic acid; 4-Vinylguaiacol
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Funding
- University Grants Commission, Government of India [40-182/2011 (SR)]
- departmental level assistance programmes UGC-SAP-DSA-I [F.5-6/2015/DSA-I (SAP-II)]
- DST-PURSE
- DBT-BUILDER, Government of India [BT/PR12153/INF/22/200/2014]
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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.
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