Bioluminescent Probe for Monitoring Endogenous Fibroblast
Activation Protein-Alpha
Posted on 2019-11-08 - 22:30
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.
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Lin, Yuxing; Ma, Zhao; Li, Zhenzhen; Gao, Yuqi; Qin, Xiaojun; Zhang, Zheng; et al. (2019). Bioluminescent Probe for Monitoring Endogenous Fibroblast
Activation Protein-Alpha. ACS Publications. Collection. https://doi.org/10.1021/acs.analchem.9b02117
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AUTHORS (9)
YL
Yuxing Lin
ZM
Zhao Ma
ZL
Zhenzhen Li
YG
Yuqi Gao
XQ
Xiaojun Qin
ZZ
Zheng Zhang
GW
Guankai Wang
LD
Lupei Du
ML
Minyong Li
KEYWORDS
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