Fibroblast activation
protein-α (FAP), as a crucial member
of cell surface glycoprotein, highly expresses in reactive fibroblasts
of tumors and several fibrosis diseases. It is a potential target
for drug design and also reported as a prodrug strategy to increase
the therapeutic window of some anticancer agents. In this work, we
developed the first bioluminogenic probe for FAP with a limit-of-detection
of 0.254 ng/mL, which could be applied to evaluate the FAP inhibitors
in vitro. The experiments of transgenic mice and tumor-bearing nude
mice validated our probe 1 could reflect the endogenous FAP level
in vivo. Furthermore, this probe was successfully used to reflect
FAP up-regulation in the lung homogenates of the bleomycin-induced
idiopathic pulmonary fibrosis mice.