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

Abstract

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, [64Cu]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 [64Cu]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 [64Cu]CM-2. Furthermore, the matched physical and biological half-life of [64Cu]CM-2 makes it a state-of-the-art PET tracer for CD133. Therefore, [64Cu]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.

• Authors: Kuan Hu, Xiaohui Ma, Lin Xie, Yiding Zhang, Masayuki Hanyu, Honoka Obata, Lulu Zhang, Kotaro Nagatsu, Hisashi Suzuki, Rui Shi, Weizhi Wang, Ming-Rong Zhang
• Journal: ACS omega (ACS Omega) Vol. 7 Issue 1 Pg. 334-341 (Jan 11 2022) ISSN: 2470-1343 [Electronic] United States
• PMID: 35036703 (Publication Type: Journal Article)
• Copyright: © 2021 The Authors. Published by American Chemical Society.