Chlorotoxin-derived bicyclic peptides for targeted imaging of glioblastomas

Meiqing Li; Ximing Shao; Chunlei Wu; Danyi Lu; Ke Liu; Wei Wang; Jiakai Liu; Hongchang Li; Wu Su; Lijing Fang

doi:10.1039/D0CC01089H

Chlorotoxin-derived bicyclic peptides for targeted imaging of glioblastomas†

Meiqing Li,‡^ab Ximing Shao,‡^a Chunlei Wu,‡^a Danyi Lu,^a Ke Liu,^a Wei Wang,^a Jiakai Liu,^a Hongchang Li,*^a Wu Su

*^a and Lijing Fang

*^ab

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* Corresponding authors

^a Guangdong Key Laboratory of Nanomedicine, Institute of Biomedicine and Biotechnology, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China
E-mail: hc.li@siat.ac.cn, wu.su@siat.ac.cn, lj.fang@siat.ac.cn

^b University of Chinese Academy of Sciences, Beijing 100049, China

Abstract

A convenient and efficient strategy was developed for accessing chlorotoxin-derived bicyclic peptide-biomolecule conjugates by cyclizing fully-unprotected linear peptides with a designed tetrafunctional chemical linker. Among these peptides, bicycle-P3 bearing the N-terminal sequence of chlorotoxin shows high tumor selectivity and penetration ability, which is promising for treatment of gliomas.

Chemical Communications

Chlorotoxin-derived bicyclic peptides for targeted imaging of glioblastomas†

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Chlorotoxin-derived bicyclic peptides for targeted imaging of glioblastomas

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