Issue 86, 2019

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

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

Supplementary files

Article information

Article type
Communication
Submitted
02 Sep 2019
Accepted
02 Oct 2019
First published
02 Oct 2019

Chem. Commun., 2019,55, 12932-12935

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, 55, 12932 DOI: 10.1039/C9CC06734E

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