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Title: In vivo covalent cross-linking of photon-converted rare-earth nanostructures for tumour localization and theranostics
Authors: Ai, Xiangzhao
Ho, Chris Jun Hui
Aw, Junxin
Attia, Amalina Binte Ebrahim
Mu, Jing
Wang, Yu
Wang, Xiaoyong
Wang, Yong
Liu, Xiaogang
Chen, Huabing
Gao, Mingyuan
Chen, Xiaoyuan
Yeow, Edwin Kok Lee
Liu, Gang
Olivo, Malini
Xing, Bengang
Keywords: Biomaterials
Drug Delivery
Issue Date: 2016
Source: Ai, X., Ho, C. J. H., Aw, J., Attia, A. B. E., Mu, J., Wang, Y., . . . Xing, B. (2016). In vivo covalent cross-linking of photon-converted rare-earth nanostructures for tumour localization and theranostics. Nature Communications, 7, 10432-. doi:10.1038/ncomms10432
Series/Report no.: Nature Communications
Abstract: The development of precision nanomedicines to direct nanostructure-based reagents into tumour-targeted areas remains a critical challenge in clinics. Chemical reaction-mediated localization in response to tumour environmental perturbations offers promising opportunities for rational design of effective nano-theranostics. Here, we present a unique microenvironment-sensitive strategy for localization of peptide-premodified upconversion nanocrystals (UCNs) within tumour areas. Upon tumour-specific cathepsin protease reactions, the cleavage of peptides induces covalent cross-linking between the exposed cysteine and 2-cyanobenzothiazole on neighbouring particles, thus triggering the accumulation of UCNs into tumour site. Such enzyme-triggered cross-linking of UCNs leads to enhanced upconversion emission upon 808 nm laser irradiation, and in turn amplifies the singlet oxygen generation from the photosensitizers attached on UCNs. Importantly, this design enables remarkable tumour inhibition through either intratumoral UCNs injection or intravenous injection of nanoparticles modified with the targeting ligand. Our strategy may provide a multimodality solution for effective molecular sensing and site-specific tumour treatment.
DOI: 10.1038/ncomms10432
Schools: School of Physical and Mathematical Sciences 
Rights: © 2016 The Author(s) (Published by Nature Publishing Group). This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SPMS Journal Articles

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