Abstract
Bromodomain and extra-terminal domain (BET) family proteins have become a hot research area because of their close relationship with a variety of human diseases. The non-invasive imaging technique, such as positron emission tomography (PET), provides a powerful tool to visualize and quantify the BET family proteins that accelerating the investigation of this domain. Herein, we describe the development of a promising PET probe, [11C]1, specifically targeting BET family proteins based on the potent BET inhibitor CF53. [11C]1 was successfully radio-synthesized with good yield and high purity after the optimization of radiolabeling conditions. The in vivo bio-activities evaluation of [11C]1 was performed using PET imaging in rodents. The results demonstrated that [11C]1 has favorable uptake in peripheral organs and moderate uptake in the brain. Further blocking studies indicated the high binding specificity and selectivity for BET proteins of this probe. Our findings suggest that [11C]1 is a promising BET PET probe for BET proteins as well as epigenetic imaging.
Highlights
The molecular imaging technique is one of the most advanced methods that has been used and integrated into various stages of the pipeline for biomedical research (Phelps, 2000; Ametamey et al, 2008)
The utilization of the molecular imaging technique allows us to understand the biological mechanisms of proteins/receptors in a more comprehensive way than the traditional in vitro techniques
The application of positron emission tomography (PET) imaging into epigenetic research would be a great benefit for many aspects of this domain
Summary
The molecular imaging technique is one of the most advanced methods that has been used and integrated into various stages of the pipeline for biomedical research (Phelps, 2000; Ametamey et al, 2008). Positron emission tomography (PET), a non-invasive imaging technique with high sensitivity as well as quantitation capability, is widely used in both clinical and research aspects. With a suitable imaging agent, PET can visualize the biomedical information and quantitatively measure the function of proteins and cellular processes in living subjects in a way that has never been done before (Alavi et al, 2004; Serdons et al, 2009). The application of PET imaging into epigenetic research would be a great benefit for many aspects of this domain
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