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Adv Mater. 2018 May;30(22):e1800106. doi: 10.1002/adma.201800106. Epub 2018 Apr 23.

Molecular Cancer Imaging in the Second Near-Infrared Window Using a Renal-Excreted NIR-II Fluorophore-Peptide Probe.

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CAS Key Laboratory of Standardization and Measurement for Nanotechnology, CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, CAS Center for Excellence in Nanoscience, National Center for Nanoscience and Technology of China, Beijing, 100190, China.
Department of Chemistry, Stanford University, Stanford, CA, 94305, USA.
Department of Materials Science and Engineering, South University of Science and Technology of China, Shenzhen, 518055, China.
Institute of Chemistry, Chinese Academy of Sciences, Beijing, 100190, China.
Sino-Danish College, University of Chinese Academy of Sciences, Beijing, 100049, China.
Center for Neuroscience Research, School of Basic Medical Sciences, Fujian Medical University, Fuzhou, 350108, China.


In vivo molecular imaging of tumors targeting a specific cancer cell marker is a promising strategy for cancer diagnosis and imaging guided surgery and therapy. While targeted imaging often relies on antibody-modified probes, peptides can afford targeting probes with small sizes, high penetrating ability, and rapid excretion. Recently, in vivo fluorescence imaging in the second near-infrared window (NIR-II, 1000-1700 nm) shows promise in reaching sub-centimeter depth with microscale resolution. Here, a novel peptide (named CP) conjugated NIR-II fluorescent probe is reported for molecular tumor imaging targeting a tumor stem cell biomarker CD133. The click chemistry derived peptide-dye (CP-IRT dye) probe afforded efficient in vivo tumor targeting in mice with a high tumor-to-normal tissue signal ratio (T/NT > 8). Importantly, the CP-IRT probes are rapidly renal excreted (≈87% excretion within 6 h), in stark contrast to accumulation in the liver for typical antibody-dye probes. Further, with NIR-II emitting CP-IRT probes, urethra of mice can be imaged fluorescently for the first time noninvasively through intact tissue. The NIR-II fluorescent, CD133 targeting imaging probes are potentially useful for human use in the clinic for cancer diagnosis and therapy.


molecular imaging; peptide probe; renal-excretion; second near-infrared window; tumor targeting

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