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

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.

MeSH terms

  • Animals
  • Blood-Testis Barrier / metabolism
  • Brain / diagnostic imaging*
  • Brain / metabolism
  • Carbon Radioisotopes / chemistry
  • Crystallography, X-Ray
  • Kinetics
  • Macaca
  • Mice
  • Molecular Conformation
  • Nerve Tissue Proteins / chemistry
  • Neurons
  • Positron-Emission Tomography*
  • Protein Domains
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / metabolism
  • Receptors, Cell Surface / chemistry


  • Carbon Radioisotopes
  • Carbon-11
  • Dner protein, mouse
  • Nerve Tissue Proteins
  • Radiopharmaceuticals
  • Receptors, Cell Surface