Bioluminescent Probe for Monitoring Endogenous Fibroblast Activation Protein-Alpha

Published on 2019-11-08T22:30:18Z (GMT) by
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