Bioluminescent Probe for Monitoring Endogenous Fibroblast Activation Protein-Alpha.
Yuxing LinZhao MaZhenzhen LiYuqi GaoXiaojun QinZheng ZhangGuankai WangLupei DuMingliang YuanPublished in: Analytical chemistry (2019)
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.
Keyphrases
- idiopathic pulmonary fibrosis
- living cells
- quantum dots
- cell surface
- high fat diet induced
- protein protein
- drug induced
- high glucose
- binding protein
- interstitial lung disease
- diabetic rats
- risk assessment
- type diabetes
- cancer therapy
- human health
- skeletal muscle
- endothelial cells
- small molecule
- insulin resistance
- drug delivery
- metabolic syndrome
- pulmonary fibrosis
- sensitive detection
- adverse drug
- climate change