Peptide-Conjugated Long-Lived Theranostic Imaging for Targeting GRPr in Cancer and Immune Cells

Wanhe Wang, Ke Jia Wu, Kasipandi Vellaisamy, Chung Hang Leung*, Edmond Dik Lung MA*

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

43 Citations (Scopus)


Gastrin-releasing peptide receptor (GRPr) plays proliferative and inflammatory roles in living systems. Here, we report a highly selective GRPr antagonist (JMV594)-tethered iridium(III) complex for probing GRPr in living cancer cells and immune cells. This probe exhibited desirable photophysical properties and also displayed negligible cytotoxicity, overcoming the inherent toxicity of the iridium(III) complex. Its long emission lifetime enabled its luminescence signal to be readily distinguished from the interfering fluorescence of organic dyes by using a time-resolved technique. This probe selectively visualized living cancer cells via specific binding to GRPr, while it also modulated the function of GRPr on TNF-α secretion in immune cells. To our knowledge, this is the first peptide-conjugated iridium(III) complex developed as a GRPr bioimaging probe and modulator of GRPr activity. This theranostic agent shows great potential at unmasking the diverse roles of GRPr in living systems.

Original languageEnglish
Pages (from-to)17897-17902
Number of pages6
JournalAngewandte Chemie. International Edition
Issue number41
Early online date10 Jul 2020
Publication statusPublished - 5 Oct 2020

Scopus Subject Areas

  • Catalysis
  • Chemistry(all)

User-Defined Keywords

  • gastrin-releasing peptide receptor (GRPr)
  • peptide-conjugated transition-metal complexes
  • theranostic agents
  • time-resolved emission spectroscopy


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