Send to

Choose Destination
Nat Commun. 2016 Jan 20;7:10432. doi: 10.1038/ncomms10432.

In vivo covalent cross-linking of photon-converted rare-earth nanostructures for tumour localization and theranostics.

Author information

Division of Chemistry and Biological Chemistry, School of Physical and Mathematical Sciences, Nanyang Technological University, 637371 Singapore, Singapore.
Singapore Bioimaging Consortium, Agency for Science Technology and Research (A*STAR), 138667 Singapore, Singapore.
Department of Chemistry, National University of Singapore, 117543 Singapore, Singapore.
State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, Center for Molecular Imaging and Translational Medicine, School of Public Health, Xiamen University, 361102 Xiamen, China.
School of Radiation Medicine and Protection, Soochow University, 215123 Suzhou, China.
Institute of Materials Research and Engineering, A*STAR (Agency for Science, Technology and Research), 117602 Singapore, Singapore.


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.

[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for Nature Publishing Group Icon for PubMed Central
Loading ...
Support Center