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Molecules 2018, 23(2), 502;

Pilot Study of 64CuCl2 for PET Imaging of Inflammation

Department of Nuclear Medicine, Shanghai Pulmonary Hospital, Tongji University School of Medicine, Shanghai 200433, China
Molecular Imaging Program at Stanford (MIPS), Department of Radiology and Bio-X Program, Canary Center at Stanford for Cancer Early Detection, Stanford University, Stanford, CA 94305-5484, USA
Institute of Clinical Science, Zhongshan Hospital, Fudan University, Shanghai 200032, China
CAS Key Laboratory of Receptor Research, Synthetic Organic & Medicinal Chemistry Laboratory (SOMCL), Shanghai Institute of Materia Medica, Chinese Academy of Sciences, No. 555 Zuchong Road, Pudong New Area, Shanghai 201203, China
Authors to whom correspondence should be addressed.
Received: 21 January 2018 / Revised: 18 February 2018 / Accepted: 20 February 2018 / Published: 24 February 2018
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Copper(II) ion (Cu2+) is the essential element for numerous pathophysiological processes in vivo. Copper transporter 1 (CTR1) is mainly responsible for maintaining Cu2+ accumulation in cells, which has been found to be over-expressed in inflammatory tissues. Therefore, we explored the potential application of 64CuCl2 for PET imaging of inflammation through targeting CTR1. The animal models of H2O2 induced muscle inflammation and lipopolysaccaharide induced lung inflammation were successfully established, then imaged by small animal PET (PET/CT) post-injection of 64CuCl2, and PET images were quantitatively analyzed. H&E and immunohistochemical (IHC) staining and western blot experiments were performed for evaluating CTR1 levels in the inflammatory and control tissues. Both inflammatory muscle and lungs can be clearly imaged by PET. PET image quantitative analysis revealed that the inflammatory muscle and lungs showed significantly higher 64Cu accumulation than the controls, respectively (p < 0.05). Furthermore, IHC staining and western blot analysis demonstrated that compared with the controls, CTR1 expression was increased in both the inflammatory muscle and lungs, which was consistent with the levels of 64Cu2+ accumulation in these tissues. 64CuCl2 can be used as a novel, simple, and highly promising PET tracer for CTR1 targeted imaging of inflammation. View Full-Text
Keywords: 64CuCl2; copper transporter 1 (CTR1); PET; inflammation 64CuCl2; copper transporter 1 (CTR1); PET; inflammation

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Jiang, L.; Song, D.; Chen, H.; Zhang, A.; Wang, H.; Cheng, Z. Pilot Study of 64CuCl2 for PET Imaging of Inflammation. Molecules 2018, 23, 502.

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