10.1021/acs.analchem.9b02117.s001 Yuxing Lin Yuxing Lin Zhao Ma Zhao Ma Zhenzhen Li Zhenzhen Li Yuqi Gao Yuqi Gao Xiaojun Qin Xiaojun Qin Zheng Zhang Zheng Zhang Guankai Wang Guankai Wang Lupei Du Lupei Du Minyong Li Minyong Li Bioluminescent Probe for Monitoring Endogenous Fibroblast Activation Protein-Alpha American Chemical Society 2019 FAP level Monitoring Endogenous Fibroblast Activation Protein-Alpha Fibroblast activation protein -α lung homogenates cell surface glycoprotein drug design fibrosis mice anticancer agents FAP up-regulation bioluminogenic probe Bioluminescent Probe FAP inhibitors bleomycin-induced idiopathic probe 1 reactive fibroblasts fibrosis diseases prodrug strategy 2019-11-08 22:30:17 Journal contribution https://acs.figshare.com/articles/journal_contribution/Bioluminescent_Probe_for_Monitoring_Endogenous_Fibroblast_Activation_Protein-Alpha/10278026 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.