A long-lived peptide-conjugated iridium(iii) complex as a luminescent probe and inhibitor of the cell migration mediator, formyl peptide receptor 2

Kasipandi Vellaisamy, Guodong Li, Wanhe Wang, Chung Hang Leung*, Edmond Dik Lung MA

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

37 Citations (Scopus)

Abstract

Formyl peptide receptors play important biological and therapeutic roles in wound repair and inflammatory diseases. In this work, we present a luminescent iridium(iii) complex (6) conjugated with the peptide agonist WKYMVm as a luminescent formyl peptide receptor 2 (FPR2) imaging probe in living cells. Complex 6 displayed ideal cell imaging characteristics, high photostability and low cytotoxicity. Competition assays with a known FPR2 antagonist, WRW4, and siRNA knockdown experiments both revealed that complex 6 selectively targeted FPR2 in living HUVEC cells. Moreover, complex 6 regulated FPR2 signalling in HUVEC cells as shown using a mechanical scratch assay. Finally, complex 6 reduced epithelial cell migration capacity and inhibited lipoxin A4 (LXA4)-triggered cell migration in HUVEC cells, demonstrating the ability of this complex to inhibit FPR2 in living cells. To our knowledge, this is the first long-lived probe for imaging FPR2 in living cells.

Original languageEnglish
Pages (from-to)8171-8177
Number of pages7
JournalChemical Science
Volume9
Issue number43
DOIs
Publication statusPublished - 2018

Scopus Subject Areas

  • Chemistry(all)

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