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.

溴结构域和末端外结构域（BET）家族蛋白由于与人类疾病的密切关系而成为研究的热点。非侵入性成像技术，例如正电子发射断层扫描（PET），提供了强大的工具来可视化和量化BET家族蛋白，从而加速了对该域的研究。在此，我们描述了有前途的PET探针的开发，[¹¹C] 1，以有效的BET抑制剂CF53为基础，专门针对BET家族蛋白。 [¹¹C] 1优化了放射性标记条件后，成功地以良好的收率和高纯度进行了放射性合成。的体内 生物活性评价 [¹¹C] 1使用PET成像在啮齿动物中进行。结果表明[¹¹C] 1对周围器官的摄取良好，对大脑的摄取适度。进一步的阻断研究表明该探针对BET蛋白具有很高的结合特异性和选择性。我们的发现表明[¹¹C] 1 是用于BET蛋白以及表观遗传学成像的有前途的BET PET探针。