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A Multifunctional Peptide‐Conjugated AIEgen for Efficient and Sequential Targeted Gene Delivery into the Nucleus
Author(s) -
Cheng Yong,
Sun Chunli,
Liu Rui,
Yang Juliang,
Dai Jun,
Zhai Tianyou,
Lou Xiaoding,
Xia Fan
Publication year - 2019
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201901527
Subject(s) - gene delivery , oligonucleotide , cytoplasm , nucleus , chemistry , genetic enhancement , peptide , conjugated system , in vivo , rna interference , gene , microbiology and biotechnology , biophysics , cancer research , biochemistry , biology , rna , genetics , organic chemistry , polymer
Gene therapy has immense potential as a therapeutic approach to serious diseases. However, efficient delivery and real‐time tracking of gene therapeutic agents have not been solved well for successful gene‐based therapeutics. Herein we present a versatile gene‐delivery strategy for efficient and visualized delivery of therapeutic genes into the targeted nucleus. We developed an integrin‐targeted, cell‐permeable, and nucleocytoplasmic trafficking peptide‐conjugated AIEgen named T D NCP for the efficient and sequential targeted delivery of an antisense single‐stranded DNA oligonucleotide (ASO) and tracking of the delivery process into the nucleus. As compared with T D NCP/siRNA‐NPs (siRNA functions mainly in the cytoplasm), T D NCP/ASO‐NPs (ASO functions mainly in the nucleus) exhibited a better interference effect, which further indicates that T D NCP is a nucleus‐targeting vector. Moreover, T D NCP/ASO‐NPs showed a favorable tumor‐suppressive effect in vivo.