Development of a CCR2 targeted 18F-labeled radiotracer for atherosclerosis imaging with PET

Xiaohui Zhang, Lin Qiu, Debbie H. Sultan, Hannah P. Luehmann, Yanbo Yu, Xiuli Zhang, Gyu Seong Heo, Alexandria Li, Divangana Lahad, Shinji Rho, Zhude Tu, Yongjian Liu

Research output: Contribution to journalArticlepeer-review


Atherosclerosis is a chronic inflammatory disease and the leading cause of morbidity and mortality worldwide. C–C motif chemokine ligand 2 and its corresponding cognate receptor 2 (CCL2/CCR2) signaling has been implicated in regulating monocyte recruitment and macrophage polarization during inflammatory responses that plays a pivotal role in atherosclerosis initiation and progression. In this study, we report the design and synthesis of a novel 18F radiolabeled small molecule radiotracer for CCR2-targeted positron emission tomography (PET) imaging in atherosclerosis. The binding affinity of this radiotracer to CCR2 was evaluated via in vitro binding assay using CCR2+ membrane and cells. Ex vivo biodistribution was carried out in wild type mice to assess radiotracer pharmacokinetics. CCR2 targeted PET imaging of plaques was performed in two murine atherosclerotic models. The sensitive detection of atherosclerotic lesions highlighted the potential of this radiotracer for CCR2 targeted PET and warranted further optimization.

Original languageEnglish
Article number108893
JournalNuclear Medicine and Biology
StatePublished - Mar 1 2024


  • Atherosclerosis
  • CCR2
  • F radiolabeling
  • Macrophages
  • PET/CT


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