Issue 80, 2020

Facile one-pot synthesis of cyclic peptide-conjugated photosensitisers for targeted photodynamic therapy

Abstract

A novel synthetic strategy for in situ cyclisation of peptides and conjugation with functional boron dipyrromethenes (BODIPYs) has been developed. Linear peptides with up to 16 amino acid residues can be cyclised effectively and the resulting conjugates can be isolated in higher than 20% yield. One of the conjugates having a cyclic RGD moiety has been studied both in vitro and in vivo. It exhibits high and selective affinity towards the αvβ3-positive cell lines and induces high photocytotoxicity. The conjugate can also selectively localise in and effectively inhibit the growth of αvβ3-overexpressed tumour in vivo.

Graphical abstract: Facile one-pot synthesis of cyclic peptide-conjugated photosensitisers for targeted photodynamic therapy

Supplementary files

Article information

Article type
Communication
Submitted
02 Leq 2020
Accepted
07 Way 2020
First published
07 Way 2020

Chem. Commun., 2020,56, 11941-11944

Facile one-pot synthesis of cyclic peptide-conjugated photosensitisers for targeted photodynamic therapy

J. C. H. Chu, C. Yang, W. Fong, C. T. T. Wong and D. K. P. Ng, Chem. Commun., 2020, 56, 11941 DOI: 10.1039/D0CC05264G

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