Targeted peptide-Au cluster binds to epidermal growth factor receptor (EGFR) in both active and inactive states : a clue for cancer inhibition through dual pathways

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journalpeer-review

8 Scopus Citations
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Author(s)

  • Peng Zhang
  • Xueyun Gao
  • Hongkang Zhao
  • Wenyong Su
  • Lina Zhao

Detail(s)

Original languageEnglish
Pages (from-to)349-355
Journal / PublicationScience Bulletin
Volume63
Issue number6
Online published8 Feb 2018
Publication statusPublished - 30 Mar 2018
Externally publishedYes

Abstract

The epidermal growth factor receptor (EGFR) has become an important target protein in anticancer drug development. Meanwhile, peptide-Au cluster has been proposed as potential targeted nano-drug assembled by targeting peptide. Here, we designed and synthesized a novel peptide-Au cluster as Au10Peptide5 to target to EGFR. We found Au10Peptide5 could target to the natural binding sites of all EGFRs at membrane in both active and inactive states by molecular simulations. Its targeted ability was further verified by the co-localization and blocking experiments. We also study the configuration modifications of both active and inactive EGFRs after binding by Au10Peptide5. For active EGFR, the absorbed Au10Peptide5 might replace the natural ligand in EGFR endocytosis process. Then, the peptide-Au cluster in endochylema could inhibit the cancer relating enzyme activity including thioredoxin reductase1 (TrxR1) and induce the oxidative stress mediated apoptosis in tumor cells. For inactive EGFR, it was retained in inactive state by Au10Peptide5 binding to inhibit dimerization of EGFR for anticancer. Both pathways might be applied in anticancer drug development based on the theoretical and experimental study here.

Research Area(s)

  • Anticancer, EGFR, peptide-Au cluster, Targeted binding

Citation Format(s)

Targeted peptide-Au cluster binds to epidermal growth factor receptor (EGFR) in both active and inactive states : a clue for cancer inhibition through dual pathways. / Zhang, Peng; Zhai, Jiao; Gao, Xueyun; Zhao, Hongkang; Su, Wenyong; Zhao, Lina.

In: Science Bulletin, Vol. 63, No. 6, 30.03.2018, p. 349-355.

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journalpeer-review