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Development of a Stable Peptide-Based PET Tracer for Detecting CD133-Expressing Cancer Cells

[Image: see text] CD133 has been recognized as a prominent biomarker for cancer stem cells (CSCs), which promote tumor relapse and metastasis. Here, we developed a clinically relevant, stable, and peptide-based positron emission tomography (PET) tracer, [(64)Cu]CM-2, for mapping CD133 protein in sev...

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Detalles Bibliográficos
Autores principales: Hu, Kuan, Ma, Xiaohui, Xie, Lin, Zhang, Yiding, Hanyu, Masayuki, Obata, Honoka, Zhang, Lulu, Nagatsu, Kotaro, Suzuki, Hisashi, Shi, Rui, Wang, Weizhi, Zhang, Ming-Rong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8756568/
https://www.ncbi.nlm.nih.gov/pubmed/35036703
http://dx.doi.org/10.1021/acsomega.1c04711
Descripción
Sumario:[Image: see text] CD133 has been recognized as a prominent biomarker for cancer stem cells (CSCs), which promote tumor relapse and metastasis. Here, we developed a clinically relevant, stable, and peptide-based positron emission tomography (PET) tracer, [(64)Cu]CM-2, for mapping CD133 protein in several kinds of cancers. Through the incorporation of a 6-aminohexanoic acid (Ahx) into the N terminus of a CM peptide, we constructed a stable peptide tracer [(64)Cu]CM-2, which exhibited specific binding to CD133-positive CSCs in multiple preclinical tumor models. Both PET imaging and ex vivo biodistribution verified the superb performance of [(64)Cu]CM-2. Furthermore, the matched physical and biological half-life of [(64)Cu]CM-2 makes it a state-of-the-art PET tracer for CD133. Therefore, [(64)Cu]CM-2 PET may not only enable the longitudinal tracking of CD133 dynamics in the cancer stem cell niche but also provide a powerful and noninvasive imaging tool to track down CSCs in refractory cancers.