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Abstract
A multifunctional photodynamic molecular beacon (PMB) has been designed and synthesized which contains an epidermal growth factor receptor (EGFR)-targeting cyclic peptide and a trimeric phthalocyanine skeleton in which the three zinc(II) phthalocyanine units are each substituted with a glutathione (GSH)-responsive 2,4-dinitrobenzenesulfonate (DNBS) quencher and are linked via two cathepsin B-cleavable GFLG peptide chains. This tailor-made conjugate is fully quenched in the native form due to the photoinduced electron transfer effect of the DNBS moieties and the self-quenching of the phthalocyanine units. It can target the EGFR overexpressed in cancer cells, and after receptor-mediated endocytosis, it can be activated selectively by the co-existence of intracellular GSH and cathepsin B, both of which are also overproduced in cancer cells, in terms of fluorescence emission and singlet oxygen generation. The cell-selective behavior of this PMB has been demonstrated using a range of cancer cells with different expression levels of EGFR, while the stimuli-responsive properties have been studied both in vitro and in various aqueous media. The overall results show that this advanced PMB, which exhibits several levels of control of the tumor specificity, is a promising photosensitizer for precise antitumoral photodynamic therapy.
| Original language | English |
|---|---|
| Article number | e202201652 |
| Journal | Chemistry - A European Journal |
| Volume | 28 |
| Issue number | 57 |
| Online published | 18 Jul 2022 |
| DOIs | |
| Publication status | Published - 12 Oct 2022 |
Funding
This work was supported by a General Research Fund from the Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No. 11303517).
Research Keywords
- cathepsin B
- epidermal growth factor receptor
- glutathione
- photodynamic therapy
- PHOTOSENSITIZERS
- DESIGN
- PHTHALOCYANINE
- DELIVERY
- CANCER
- LOCK
Publisher's Copyright Statement
- COPYRIGHT TERMS OF DEPOSITED POSTPRINT FILE: This is the peer reviewed version of the following article: Tam, L. K. B., He, L., Ng, D. K. P., Cheung, P. C. K., & Lo, P-C. (2022). A Tumor-Targeting Dual-Stimuli-Activatable Photodynamic Molecular Beacon for Precise Photodynamic Therapy. Chemistry - A European Journal, 28(57), [e202201652], which has been published in final form at https://doi.org/10.1002/chem.202201652.
- This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions. This article may not be enhanced, enriched or otherwise transformed into a derivative work, without express permission from Wiley or by statutory rights under applicable legislation. Copyright notices must not be removed, obscured or modified. The article must be linked to Wiley’s version of record on Wiley Online Library and any embedding, framing or otherwise making available the article or pages thereof by third parties from platforms, services and websites other than Wiley Online Library must be prohibited.
RGC Funding Information
- RGC-funded
Fingerprint
Dive into the research topics of 'A Tumor-Targeting Dual-Stimuli-Activatable Photodynamic Molecular Beacon for Precise Photodynamic Therapy'. Together they form a unique fingerprint.Projects
- 1 Finished
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GRF: Development of Advanced Photodynamic Molecular Beacons with Multiple Controls for Targeted Photodynamic Therapy
LO, P. C. (Principal Investigator / Project Coordinator) & CHIN, R. Y. M. (Co-Investigator)
1/01/18 → 17/06/22
Project: Research