1. FAP-Targeted Fluorescent Imaging Agents to Study Cancer-Associated Fibroblasts In Vivo.
- Author
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Deutsch-Williams RJ, Schleyer KA, Das R, Carrothers JE, Kohler RH, Vinegoni C, and Weissleder R
- Subjects
- Animals, Humans, Mice, Optical Imaging methods, Cell Line, Tumor, Quinolones chemistry, Neoplasms diagnostic imaging, Neoplasms drug therapy, Neoplasms metabolism, Neoplasms pathology, Fluorescent Dyes chemistry, Gelatinases metabolism, Endopeptidases metabolism, Serine Endopeptidases metabolism, Membrane Proteins metabolism, Cancer-Associated Fibroblasts metabolism, Cancer-Associated Fibroblasts drug effects
- Abstract
Cancer-associated fibroblasts (CAFs) expressing fibroblast activation protein alpha (FAP) are abundant in tumor microenvironments and represent an emerging target for PET cancer imaging. While different quinolone-based small molecule agents have been developed for whole-body imaging, there is a scarcity of well-validated fluorescent small molecule imaging agents to better study these cells in vivo. Here, we report the synthesis and characterization of a series of fluorescent FAP imaging agents based on the common quinolone azide inhibitor. Our data show excellent performance of some synthesized FAP Targeting Fluorescent probes (FTFs) for both topical application and intravenous delivery to label CAF populations in solid tumors. These results suggest that FTF can be used to study CAF biology and therapeutic targeting in vivo.
- Published
- 2025
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