biostudies-literatureZhang XNIBIB NIH HHSNHLBINHLBI NIH HHSNational Cancer InstituteNINDS NIH HHSNCI NIH HHSNational Institutes of HealthNIBIBMallinckrodt Institute of RadiologyNIH HHSNINDS108893https://www.ebi.ac.uk/biostudies/studies/S-EPMC10964492biostudies-literatureUnknown130-131Atherosclerosis is a chronic inflammatory disease and the leading cause of morbidity and mortality worldwide. CC 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.Nuclear medicine and biologyDevelopment of a CCR2 targeted ¹⁸F-labeled radiotracer for atherosclerosis imaging with PET.PMC10964492R01 HL151685R01NS103988R01 HL150891R01 NS103988S10 OD030403S10OD030403R01 HL153436S10OD018515R35 HL145212R01NS075527P30CA091842S10 OD018515R01HL151685R01 NS075527P30 CA091842P41EB025815P41 EB025815Liu YLuehmann HPHeo GSZhang XRho SLi ASultan DHLahad DTu ZQiu LYu YfalseDevelopment of a CCR2 targeted ¹⁸F-labeled radiotracer for atherosclerosis imaging with PET.Atherosclerosis is a chronic inflammatory disease and the leading cause of morbidity and mortality worldwide. CC 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.2024-01-01T00:00:00Z2024 Mar-Apr2025-04-22T18:48:46.458Z2025-04-06T02:38:11.45ZS-EPMC109644923842291810.1016/j.nucmedbio.2024.108893