正电子发射断层扫描探针靶向溴结构域和末端（BET）结构域，以实现体内神经表观遗传学成像。
Positron emission tomography probes targeting bromodomain and extra-terminal (BET) domains to enable in vivo neuroepigenetic imaging.
机构信息
Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, P. R. China.
Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA.
出版信息
Chem Commun (Camb). 2019 Oct 24;55(86):12932-12935. doi: 10.1039/c9cc06734e.
Here, we report the development of novel PET radiotracer ([11C]CW22) of BET proteins. In vivo imaging results in rodents and nonhuman primates (NHP) demonstrate that [11C]CW22 has excellent brain uptake, good specificity, good selectivity, suitable metabolism, appropriate kinetics and distribution in the brain. Our studies demonstrated that [11C]CW22 exhibits ideal properties as a PET imaging probe of BET proteins for further validation.
在这里，我们报告了新型 BET 蛋白 PET 放射性示踪剂 ([11C]CW22) 的开发。在啮齿动物和非人类灵长类动物 (NHP) 中的体内成像结果表明，[11C]CW22 具有优异的脑摄取、良好的特异性、良好的选择性、合适的代谢、适当的脑内动力学和分布。我们的研究表明，[11C]CW22 作为 BET 蛋白的 PET 成像探针具有理想的特性，有待进一步验证。
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