Chemoselective reactions are important strategies for the covalent attachment of functional entities to biomolecules to create novel constructs for biological applications. In this work, we modified cyclometalated iridium(III) polypyridine complexes with a perfluorobiphenyl (PFBP) moiety to afford novel biological reagents for bioconjugation, bioimaging, and phototherapeutic applications. Reactions of the PFBP complexes with peptides containing a FCPF (pi-clamp) sequence via the selective cysteine conjugation afforded luminescent peptide conjugates that exhibited rich photophysical properties.  Importantly, the conjugation of complexes to organelle-targeting peptides was found to modulate their intracellular localization behavior, which was further shown to be important to their performance in photodynamic therapy.

Photofunctional Cyclometalated Iridium(III) Polypyridine Complexes Bearing a Perfluorobiphenyl Moiety for Bioconjugation, Bioimaging, and Phototherapeutic Applications

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