Related Experiment Video
Updated: May 28, 2026
Fluorescence Molecular Tomography for In Vivo Imaging of Glioblastoma Xenografts
Published on: April 26, 2018
Environment-sensitive fluorescent probes targeting mutant IDH1 for in vivo glioma imaging
Wenhua Li1, Luning Song2, Wenshuo Lv2
1Department of Pharmacy, The Second Qilu Hospital of Shandong University, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250033, China.
Background:
Surgery serves as a cornerstone in glioma treatment, yet achieving complete resection remains a significant challenge due to the infiltrative nature of these tumors. Microscopic residual lesions frequently lead to recurrence, whereas excessive resection risks damaging critical neurological functions. Fluorescent imaging technology enables the real-time visualization and precise delineation of glioma margins. However, commonly clinical fluorescent agents for gliomas, such as 5-ALA, fluorescein sodium, and ICG, are limited in their widespread application due to low selectivity and sensitivity. Consequently, there is a pressing need to develop novel targeted fluorescent probes capable of achieving highly specific and accurate localization of glioma tissue.
Results:
In this study, we developed a new class of small-molecule fluorescent probes targeting the glioma-associated biomarker mutant isocitrate dehydrogenase 1 (mIDH1). Through multi-level evaluation spanning protein, cellular, and in vivo models, MIP01 was identified as the optimal probe. The probe possessed high affinity (Kd = 156 ± 49.9 nM) and selectivity for mIDH1, displaying a significantly enhanced fluorescence response upon binding that enables precise labeling of glioma cells. More importantly, MIP01 demonstrated outstanding performance in orthotopic glioma xenograft models. It efficiently crossed the blood-brain barrier, selectively accumulated in tumor regions, and produced intense fluorescence signals.
Significance:
In conclusion, fluorescent probe MIP01 achieves precise glioma identification through selective mIDH1 labeling in vitro and in vivo, demonstrating considerable potential as a targeted fluorescence imaging agent for delineating tumor margins in mIDH1-positive gliomas.
Insights
A novel fluorescent probe, MIP01, targets mutant isocitrate dehydrogenase 1 (mIDH1) for precise glioma margin delineation. This targeted approach enhances visualization, improving surgical outcomes for mIDH1-positive gliomas.
Area of Science:
- Biomedical Engineering
- Molecular Imaging
- Oncology
Background:
- Glioma surgery is challenged by infiltrative tumor growth, leading to recurrence or neurological damage.
- Current fluorescent agents lack the specificity and sensitivity for accurate glioma margin detection.
- Novel targeted probes are needed for precise glioma tissue localization.
Purpose of the Study:
- To develop and evaluate a novel small-molecule fluorescent probe for targeted glioma imaging.
- To assess the probe's efficacy in identifying glioma margins by targeting mutant isocitrate dehydrogenase 1 (mIDH1).
Main Methods:
- Developed small-molecule fluorescent probes targeting mIDH1.
- Evaluated probe performance in protein, cellular, and in vivo orthotopic glioma xenograft models.
- Assessed probe affinity, selectivity, blood-brain barrier penetration, and fluorescence signal intensity.
Main Results:
- Identified MIP01 as the optimal probe with high affinity (Kd = 156 ± 49.9 nM) and selectivity for mIDH1.
- MIP01 demonstrated enhanced fluorescence upon binding, enabling precise glioma cell labeling.
- In vivo studies showed efficient blood-brain barrier crossing, selective tumor accumulation, and intense fluorescence signals.
Conclusions:
- Fluorescent probe MIP01 enables precise glioma identification via selective mIDH1 labeling.
- MIP01 shows significant potential as a targeted fluorescence imaging agent for delineating tumor margins in mIDH1-positive gliomas.
