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Published on: March 17, 2023
NIR C-Myc Pu22 G-quadruplex probe as a photosensitizer for bioimaging and antitumor study
Jun-Hui Li1, Pei-Dan You1, Fei Lu1
1Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
Abstract:
Despite the fact that C-Myc G-quadruplex in the oncogene promoter regions is one of the crucial targets of antitumor drugs, the selectivities and proliferation inhibitions of its probes towards tumor cells remain a big challenge. Until now, no effective C-Myc G-quadruplex probes have been reported as a photosensitizer to increase their antitumor activities. Here, the first NIR C-Myc G-quadruplex probe PDS-SQ has been designed, comprising a G-quadruplex binder PDS and a squaraine dye SQ as a photosensitizer. Conjugate PDS-SQ could selectively NIR image C-Myc Pu22 G-quadruplex in tumor cells, and show stronger antitumor activity in the irradiation by a chemo-photodynamic method than in the dark. The study provides a new way to develop the novel NIR C-Myc G-quadruplex probes with more potent antitumor activities.
Insights
Researchers developed a novel near-infrared (NIR) probe, PDS-SQ, for C-Myc G-quadruplex. This probe selectively images cancer cells and enhances antitumor activity via chemo-photodynamic therapy.
Area of Science:
- Medicinal Chemistry
- Oncology
- Biotechnology
Background:
- C-Myc G-quadruplex in oncogene promoter regions is a key target for antitumor drugs.
- Developing selective probes with potent antitumor activity remains a significant challenge.
- Existing C-Myc G-quadruplex probes lack photosensitizing capabilities for enhanced therapeutic effects.
Purpose of the Study:
- To design and synthesize the first near-infrared (NIR) C-Myc G-quadruplex probe.
- To evaluate the probe's selectivity, imaging capabilities, and antitumor efficacy.
- To explore a novel chemo-photodynamic therapeutic approach for cancer treatment.
Main Methods:
- Design and synthesis of a novel probe (PDS-SQ) combining a G-quadruplex binder (PDS) and a squaraine dye photosensitizer (SQ).
- Selective imaging of C-Myc Pu22 G-quadruplex in tumor cells using NIR technology.
- Assessment of antitumor activity through chemo-photodynamic therapy under irradiation versus dark conditions.
Main Results:
- The PDS-SQ probe successfully and selectively imaged C-Myc Pu22 G-quadruplex in tumor cells via NIR.
- PDS-SQ demonstrated significantly enhanced antitumor activity when combined with irradiation (chemo-photodynamic therapy) compared to dark conditions.
- The study validates the potential of PDS-SQ as a theranostic agent for C-Myc-driven cancers.
Conclusions:
- The developed NIR probe PDS-SQ offers a promising tool for selective C-Myc G-quadruplex imaging in tumor cells.
- Chemo-photodynamic therapy using PDS-SQ significantly boosts antitumor efficacy.
- This work presents a novel strategy for developing potent NIR C-Myc G-quadruplex probes for enhanced cancer treatment.
