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.