Conditional internalization of PEGylated nanomedicines by PEG engagers for triple negative breast cancer therapy

Yu Cheng Su, Pierre Alain Burnouf, Kuo Hsiang Chuang, Bing Mae Chen, Tian Lu Cheng, Steve R. Roffler

Research output: Contribution to journalArticlepeer-review

24 Citations (Scopus)

Abstract

Triple-negative breast cancer (TNBC) lacks effective treatment options due to the absence of traditional therapeutic targets. The epidermal growth factor receptor (EGFR) has emerged as a promising target for TNBC therapy because it is overexpressed in about 50% of TNBC patients. Here we describe a PEG engager that simultaneously binds polyethylene glycol and EGFR to deliver PEGylated nanomedicines to EGFR + TNBC. The PEG engager displays conditional internalization by remaining on the surface of TNBC cells until contact with PEGylated nanocarriers triggers rapid engulfment of nanocargos. PEG engager enhances the anti-proliferative activity of PEG-liposomal doxorubicin to EGFR + TNBC cells by up to 100-fold with potency dependent on EGFR expression levels. The PEG engager significantly increases retention of fluorescent PEG probes and enhances the antitumour activity of PEGylated liposomal doxorubicin in human TNBC xenografts. PEG engagers with specificity for EGFR are promising for improved treatment of EGFR + TNBC patients.

Original languageEnglish
Article number15507
JournalNature Communications
Volume8
DOIs
Publication statusPublished - Jun 8 2017

ASJC Scopus subject areas

  • Chemistry(all)
  • Biochemistry, Genetics and Molecular Biology(all)
  • Physics and Astronomy(all)

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