Advanced Fibroblast Activation Protein-Ligand Developments: FAP Imaging Agents: A Review of the Structural...

Fibroblast activation protein-α (FAP) has attracted increasing attention as a selective marker of cancer-associated fibroblasts (CAFs) and more broadly, of activated fibroblasts in tissues undergoing remodeling of their ECM due to chronic inflammation, fibrosis, or wound healing. Since FAP is critical to the initiation of metastatic growth, its expression will serve as a molecular marker to detect tumors at an earlier stage of development compared to currently available methods. The design of high affinity small molecule FAP inhibitor will allow for noninvasive imaging of activated fibroblast in cancer patients. Small molecule inhibitors of FAP are being developed for targeted radiotherapy of tumors.