ac9b02117_si_001.pdf (1.87 MB)
Bioluminescent Probe for Monitoring Endogenous Fibroblast Activation Protein-Alpha
journal contribution
posted on 2019-11-08, 22:30 authored by Yuxing Lin, Zhao Ma, Zhenzhen Li, Yuqi Gao, Xiaojun Qin, Zheng Zhang, Guankai Wang, Lupei Du, Minyong LiFibroblast 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.
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FAP levelMonitoring Endogenous Fibroblast Activation Protein-Alpha Fibroblast activation protein -αlung homogenatescell surface glycoproteindrug designfibrosis miceanticancer agentsFAP up-regulationbioluminogenic probeBioluminescent ProbeFAP inhibitorsbleomycin-induced idiopathicprobe 1reactive fibroblastsfibrosis diseasesprodrug strategy
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