Table Info

Table 3.

TSPO-targeted therapies and imaging in gliomas

Therapy	Merits	MOA	Clinical uses	Reference(s)
[¹¹C]PK11195	The high specificity for TSPO allows for tumor detection.	Binds to TSPO in the outer mitochondrial membrane, enabling PET imaging.	Imaging of TSPO-positive glioblastoma.	[86, 99]
[¹⁸F]DPA-714	It enhances imaging techniques and may reduce tumor growth.	TSPO antagonist, inhibiting tumor cell proliferation and inducing apoptosis.	Potential in clinical trials for therapy.	[36, 100, 101]
[¹⁸F]FEPPA	High sensitivity and specificity for TSPO allow the monitoring of treatment responses.	Selectively binds to TSPO in the outer mitochondrial membrane, enabling PET imaging.	Detection of TSPO-expressing gliomas and monitoring therapies.	[102, 103]
[¹⁸F]PBR111	Non-invasive imaging and quantification of TSPO expression.	Binds to TSPO and enables PET imaging of tumor viability.	Used in glioma diagnosis and assessment of treatment efficacy.	[104]
[¹¹C]PBR-28	Selectively eliminates TSPO-positive glioma cells.	Induces apoptosis in TSPO-expressing cells.	Targeted chemotherapy for treating TSPO-positive gliomas.	[102, 105]
Ro5-4864	Anti-proliferative effects in glioma cells promote apoptosis.	It inhibits TSPO, disrupting cellular metabolism and leading to cell death.	Preclinical studies focusing on glioma treatment.	[51, 106]
[¹⁸F]GE180	High binding affinity to TSPO and a better signal-to-noise ratio make it useful for distinguishing tumor types.	Binding to TSPO allows visualization of activated cells, specifically within tumor areas contributing to the glioma pathology.	Imaging of glioma to assess tumor viability and differentiate between types of gliomas based on TSPO expression.	[36, 66, 107]

[¹¹C]PBR-28: N-(2-[¹¹C]methoxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide; [¹¹C]PK11195: [¹¹C]N-butan-2-yl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide; [¹⁸F]DPA-714: [¹⁸F]N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide; [¹⁸F]FEPPA: [¹⁸F]N-(2-(2-fluoroethoxy)benzyl)-N-(4-phenoxypyridin-3-yl)acetamide; [¹⁸F]GE180: [¹⁸F]3-(2-fluoroethyl)-2-[(4-methoxyphenyl)thiomethyl]-8-methylquinazolin-4-one; [¹⁸F]PBR111: 2-(6-chloro-2-(4-(3-[¹⁸F]fluoropropoxy)phenyl)imidazo[1,2-a]pyridin-3-yl)-N,N-diethylacetamide; MOA: mechanisms of action; PET: positron emission tomography; Ro5-4868: 4'-chlorodiazepam; TSPO: translocator protein

Declarations

Acknowledgments

We acknowledge the support of the Department of Nuclear Medicine at Nanjing First Hospital.

Author contributions

JM: Writing—original draft. BL and JW: Writing—review & editing. FW: Conceptualization, Investigation, Writing—review & editing, Funding acquisition. YY: Conceptualization, Investigation, Writing—review & editing.

Conflicts of interest

The authors declare that they have no conflicts of interest.

Ethical approval

Not applicable.

Consent to participate

Not applicable.

Consent to publication

Not applicable.

Availability of data and materials

Not applicable.

Funding

The National Key Research and Development Program of China [2022YFC2406900] supports this work. The key subjects of nuclear medicine: Jiangsu Provincial Institute of Medical Sciences [JSDW202247]. Jiangsu Provincial Medical Key Discipline Cultivation Unit [JSDW202247]. Nanjing International/Hong Kong, Macao, and Taiwan Science and Technology Cooperation Program Project [202308005]. The National Natural Science Foundation of China [82301609], China Postdoctoral Science Foundation [2022M711666], Natural Science Foundation of Jiangsu Province [BK20220196], the International Joint Research and Development Project of Nanjing [202201030], and the International Joint Research and Development Project of Nanjing [202308005]. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.

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