Novel 64Cu-labeled CUDC-101 for in vivo PET imaging of histone deacetylases

Qingqing Meng, Feng Li, Sheng Jiang, Zheng Li

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

We report the design, synthesis, and biological evaluation of a 64Cu-labeled histone deacetylase (HDAC) imaging probe, which was obtained by introduction of metal chelator through click reaction of HDAC inhibitor CUDC-101 and then radiolabeled with 64Cu. The resulting 64Cu-labeled compound 7 ([64Cu]7) was identified as a positron emission tomography (PET) imaging probe to noninvasively visualize HDAC expression in vivo. Cell based competitive assay established the specific binding of [64Cu]7 to HDACs. Biodistribution and small-animal microPET/CT studies further showed that [64Cu]7 had high tumor to background ratio in the MDA-MB-231 xenograft model, a triple-negative breast cancer with high expression of HDACs. To our knowledge, [64Cu]7 thus represents the first 64Cu-labeled PET HDAC imaging probe, which exhibits nanomolar range binding affinity and capability to imaging HDAC expression in triple-negative breast cancer in vivo.

Original languageEnglish (US)
Pages (from-to)858-862
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume4
Issue number9
DOIs
StatePublished - Sep 12 2013

Keywords

  • CUDC-101
  • histone deacetylases inhibitors
  • PET imaging probe
  • triple-negative breast cancer

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

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