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

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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.

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

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Publication details

The article was received on 02 Sep 2019, accepted on 02 Oct 2019 and first published on 02 Oct 2019


Article type: Communication
DOI: 10.1039/C9CC06734E
Chem. Commun., 2019, Advance Article

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

    P. Bai, H. Wey, D. Patnaik, X. Lu, Y. Lan, J. Rokka, F. Stephanie, S. J. Haggarty and C. Wang, Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9CC06734E

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