Publications Repository - Helmholtz-Zentrum Dresden-Rossendorf

Early detection and treatment of cancers can significantly increase patient prognosis and enhance the quality of life of affected patients. The emerging significance of the tumor microenvironment (TME) as a new frontier for cancer diagnosis and therapy may be exploited by radiolabeled tracers for diagnostic imaging techniques such as positron emission tomography (PET). Cancer-associated fibroblasts (CAFs) within the TME are identified by biomarkers such as fibroblast activation protein alpha (FAPα), which are expressed on their surfaces. Targeting FAPα using small molecule 18F-labeled inhibitors (FAPIs) have recently garnered significant attention for non-invasive tumor visualization using PET. Currently, the predominant 18F-fluorination method for radiolabeling FAPIs involves chelation-based radiofluorination strategies using aluminum [18F]fluoride ([18F]AlF). Herein, a powerful radiofluorination protocol for the preparation of two 18F-labeled FAPIs via the sulfur [18F]fluoride exchange ([18F]SuFEx) reaction and preliminary biological evaluation is disclosed.