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. 2019 Oct 24;55(86):12932-12935.
doi: 10.1039/c9cc06734e.

Positron emission tomography probes targeting bromodomain and extra-terminal (BET) domains to enable in vivo neuroepigenetic imaging

Ping Bai  1 , Hsiao-Ying Wey  2 , Debasis Patnaik  3 , Xiaoxia Lu  4 , Yu Lan  2 , Johanna Rokka  2 , Fiedler Stephanie  2 , Stephen J Haggarty  3 , Changning Wang  2
Affiliations

Positron emission tomography probes targeting bromodomain and extra-terminal (BET) domains to enable in vivo neuroepigenetic imaging

Ping Bai et al. Chem Commun (Camb). .

Abstract

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.

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