TY - JOUR
T1 - Development of a Stable Peptide-Based PET Tracer for Detecting CD133-Expressing Cancer Cells
AU - Hu, Kuan
AU - Ma, Xiaohui
AU - Xie, Lin
AU - Zhang, Yiding
AU - Hanyu, Masayuki
AU - Obata, Honoka
AU - Zhang, Lulu
AU - Nagatsu, Kotaro
AU - Suzuki, Hisashi
AU - Shi, Rui
AU - Wang, Weizhi
AU - Zhang, Ming Rong
N1 - Publisher Copyright:
© 2021 The Authors. Published by American Chemical Society
PY - 2022/1/11
Y1 - 2022/1/11
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85122404380&partnerID=8YFLogxK
U2 - 10.1021/acsomega.1c04711
DO - 10.1021/acsomega.1c04711
M3 - Article
AN - SCOPUS:85122404380
SN - 2470-1343
VL - 7
SP - 334
EP - 341
JO - ACS Omega
JF - ACS Omega
IS - 1
ER -
