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Updated: Jun 26, 2026
Spatiotemporally Controlled Nuclear Translocation of Guests in Living Cells Using Caged Molecular Glues as Photoactivatable Tags
Published on: January 17, 2019
AND-gate fluorescence prodrug of the self-immolative delivery for overcoming multidrug resistance
Jun Liu1, Zhengqin Liu1, Yifen Yang1
1School of Chinese Ethnic Medicine, Guizhou Minzu University, Guiyang 550025, China.
Abstract:
The principle goal of clinical tumor treatment is to improve the therapeutic outcomes in the clinic while suppressing undesired side-effects of anticancer drugs. However, its clinical usage of fluorescence prodrug was significantly hampered with some critical issues such as water-solubility, blood circulation, therapeutic efficacy, inevitable leakage, and side effects simultaneously. Herein, based on the strategy of the unique grafting structure, we report H2O2 activatable phototheranostic probes targeting the Golgi in mice with hypertension. The drug release study in vitro demonstrated that LGM-XL can diagnose cancer effectively by monitoring fluctuations of H2O2 in vivo through fluorescence imaging. More importantly, the prodrug LGM-XL could detect and image endogenous H2O2 in inflamed mice in situ, while effectively avoiding drug leakage in blood. The novel multifunctional drug delivery system enhanced not only Golgi oxidative stress in the pathophysiology of hypertension by stimulation of H2O2 but also the molecular mechanism for the diagnosis of inflamed-related diseases (e.g., drug-induced liver injury and the liver repair).
Insights
Researchers developed a novel H2O2-activatable prodrug, LGM-XL, for cancer diagnosis and treatment. This innovative probe targets the Golgi, effectively imaging hydrogen peroxide (H2O2) in vivo while minimizing side effects and drug leakage.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Clinical tumor treatment aims to enhance efficacy and reduce side effects of anticancer drugs.
- Current fluorescence prodrugs face challenges including poor water-solubility, limited circulation, leakage, and toxicity.
- Hydrogen peroxide (H2O2) is a key biomarker in various pathological conditions.
Purpose of the Study:
- To develop a H2O2-activatable phototheranostic probe for improved cancer diagnosis and therapy.
- To target the Golgi apparatus and monitor H2O2 fluctuations in vivo.
- To create a multifunctional drug delivery system that enhances therapeutic outcomes and minimizes side effects.
Main Methods:
- Design and synthesis of a novel grafting structure-based prodrug, LGM-XL.
- In vitro drug release studies to assess H2O2 responsiveness.
- In vivo fluorescence imaging in mice to monitor H2O2 levels and drug distribution.
- Evaluation of the prodrug's effect on Golgi oxidative stress and inflammatory disease models.
Main Results:
- LGM-XL effectively diagnosed cancer by monitoring H2O2 fluctuations using fluorescence imaging in vitro.
- The prodrug successfully detected and imaged endogenous H2O2 in inflamed mice in situ, preventing drug leakage.
- The drug delivery system stimulated Golgi oxidative stress and showed potential in diagnosing inflammatory diseases like drug-induced liver injury.
Conclusions:
- The H2O2-activatable phototheranostic probe LGM-XL offers a promising strategy for cancer theranostics.
- This novel system overcomes limitations of traditional prodrugs by enabling targeted H2O2 detection and controlled drug release.
- The findings highlight the potential of LGM-XL in managing inflammatory diseases and improving therapeutic outcomes.
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