Photosensitizer-conjugated tryptophan-containing peptide ligands as new dual-targeted theranostics for cancers

Jisu Kim, Jihyun Chae, Jun Soo Kim, Sung Ho Goh, Yongdoo Choi

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

Here we report that new dual-targeted theranostic anti-cancer agents can be produced by simple conjugation of photosensitizers with tryptophan-containing peptide ligands via cyclic disulfide linkages. In the proof-of-concept study, photosensitizers conjugated with EGFR-targeting peptide GE11 (C-EGFR) were in close proximity with tryptophan residues in the conjugate, resulting in quenching of its fluorescence and singlet oxygen generation. C-EGFR specifically binds to target receptors on the cancer cell surface, after which it is internalized via receptor-mediated endocytosis. Intracellular cleavage of cyclic disulfide bonds allows separation of the photosensitizers from the tryptophan residue, after which they emit near-infrared (NIR) fluorescence and produce a phototoxic effect in the target cells. This strategy enabled us to accomplish simultaneous real-time NIR fluorescence imaging of EGFR-overexpressing cancer cells with high contrast and selective photodynamic therapy

Original languageEnglish
Pages (from-to)584-590
Number of pages7
JournalInternational Journal of Pharmaceutics
Volume513
Issue number1-2
DOIs
StatePublished - 20 Nov 2016

Keywords

  • Activatable
  • EGFR target
  • Fluorescence imaging
  • Photodynamic therapy
  • Theranostics

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