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Published on: February 1, 2016
Development of New Positron Emission Tomography Radiotracer for BET Imaging
Changning Wang1, Frederick A Schroeder1, Jacob M Hooker1
1Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School , Charlestown, Massachusetts 02129, United States.
Abstract:
The bromodomain and extraterminal domain (BET) inhibitors have been extensively studied for tumor treatment in the past few years. Recently, BET-containing proteins have been reported to play a key role in brain functions, such as learning and memory. BET proteins have also been shown to be a potential therapeutic target for substance abuse disorders. Development of a molecular probe for noninvasive imaging will elucidate the distribution and functional roles of BET in the living subject and accelerate medical research and drug discovery in this domain. Herein, we describe the synthesis and pilot imaging of a novel BET imaging agent, [11C]MS417. Our imaging results demonstrate that this probe has moderate brain uptake, good specificity, good selectivity, and appropriate kinetics and distribution. [11C]MS417 is an ideal lead compound for further optimization of clinical BET PET radiotracer tools and MS417 could be used as a blood-brain-barrier-penetrant compound for preclinical research.
Insights
Researchers developed a novel Carbon-11 labeled molecular probe, [11C]MS417, for imaging bromodomain and extraterminal domain (BET) proteins in the brain. This imaging agent shows promise for understanding brain function and developing treatments for neurological disorders and substance abuse.
Area of Science:
- Neuroscience
- Pharmacology
- Radiochemistry
Background:
- Bromodomain and extraterminal domain (BET) inhibitors are investigated for cancer therapy.
- BET proteins are crucial for brain functions like learning and memory.
- BET proteins represent a therapeutic target for substance abuse disorders.
Purpose of the Study:
- To develop a molecular probe for noninvasive imaging of BET proteins in vivo.
- To elucidate the distribution and functional roles of BET proteins in living subjects.
- To accelerate medical research and drug discovery for neurological and substance abuse disorders.
Main Methods:
- Synthesis of a novel Carbon-11 labeled BET imaging agent, [11C]MS417.
- Pilot imaging studies to evaluate the probe's performance in vivo.
- Assessment of brain uptake, specificity, selectivity, kinetics, and distribution.
Main Results:
- [11C]MS417 demonstrated moderate brain uptake.
- The probe exhibited good specificity and selectivity for BET proteins.
- Kinetics and distribution of the probe were found to be appropriate for imaging.
Conclusions:
- [11C]MS417 is a promising lead compound for developing clinical BET Positron Emission Tomography (PET) radiotracers.
- MS417 can serve as a blood-brain-barrier-penetrant compound for preclinical research.
- This novel imaging agent facilitates further investigation into BET protein roles in the brain.
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