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Published on: March 16, 2018
Multifunctional Theranostic Probe Based on the Pim-1 Kinase Inhibitor with the Function of Tracking pH Fluctuations
Caiyun Liu1, Xin Wang1, Hanchuang Zhu1
1School of Water Conservancy and Environment, University of Jinan, Jinan, Shandong 250022, China.
Abstract:
Currently, kinase inhibitors have been applied in the diagnosis or treatment of cancer with their unique advantages. It is of great significance to develop some comprehensive theranostic reagents based on kinase inhibitors to improve the performance of reagents for biomedical applications. Besides, tracking changes in the intracellular environment (e.g., pH) during cancer development and drug delivery is also critical for cancer research and treatment. Therefore, it is an urgent desire to design some novel multifunctional reagents based on kinase inhibitor strategies that can trace changes in the microenvironment of cancer cells. In this paper, a multifunctional theranostic reagent based on Pim-1 kinase inhibitor 5-bromobenzofuran-2-carboxylic acid is proposed. The theranostic probe binds to tumor-specific Pim-1 kinase, releases strong fluorescence, and produces cytotoxicity, thus achieving cell screening and killing effects. Furthermore, the probe can specifically target lysosomes and sensitively respond to pH. It can be used to track the pH changes in the intracellular environment under conditions of autophagy and external stimulation, as a visual tool to monitor pH fluctuations during cancer treatment. In conclusion, this simple but multifunctional theranostic reagent proposed in this work is expected to provide a promising method for cancer diagnosis and therapy.
Insights
This study introduces a novel theranostic probe for cancer, utilizing a kinase inhibitor to target cancer cells, enabling both diagnosis and therapy. The probe also tracks intracellular pH changes, aiding cancer research and treatment monitoring.
Area of Science:
- Biomedical Engineering
- Molecular Oncology
- Chemical Biology
Background:
- Kinase inhibitors are valuable tools in cancer diagnosis and treatment.
- Developing advanced theranostic reagents is crucial for improving cancer care.
- Monitoring intracellular microenvironments, like pH, is vital for understanding cancer progression and drug efficacy.
Purpose of the Study:
- To design a multifunctional theranostic reagent based on kinase inhibitor strategies.
- To create a probe capable of targeting cancer cells and monitoring intracellular pH.
- To develop a novel tool for cancer cell screening, killing, and pH fluctuation tracking.
Main Methods:
- A novel theranostic probe was synthesized using 5-bromobenzofuran-2-carboxylic acid, a Pim-1 kinase inhibitor.
- The probe's ability to bind to tumor-specific Pim-1 kinase was investigated.
- The probe's fluorescence, cytotoxicity, lysosomal targeting, and pH responsiveness were evaluated.
Main Results:
- The developed probe exhibits specific binding to Pim-1 kinase, releasing fluorescence and inducing cytotoxicity for cancer cell screening and killing.
- The probe effectively targets lysosomes and responds sensitively to pH changes.
- It serves as a visual tool for tracking intracellular pH fluctuations during autophagy and in response to external stimuli.
Conclusions:
- A multifunctional theranostic reagent based on a Pim-1 kinase inhibitor was successfully developed.
- This reagent offers a promising approach for simultaneous cancer cell targeting, killing, and intracellular pH monitoring.
- The proposed probe is expected to advance cancer diagnosis and therapeutic strategies.
