title: A fluorescent light-up aggregation-induced emission probe for screening gefitinib-sensitive non-small cell lung carcinoma.
abstract: Fluorescent light-up probes with aggregation-induced emission (AIE) characteristics have been focused on recently. In this report, a new fluorescent probe, namely, DEVD-TPE, which consisted of the substrate peptide Asp-Glu-Val-Asp (DEVD) and the AIE reporter group tetraphenylethene (TPE), was developed for detecting caspase-3 in living cells. In a slightly alkaline solution, the DEVD-TPE probe displayed almost no fluorescence owing to the dynamic rotation of the phenyl rings in solution. However, DEVD-TPE exhibited significant fluorescence when it was cleaved by caspase-3, as well as when the reporter group TPE underwent aggregation. The epidermal growth factor receptor (EGFR) inhibitor gefitinib was used for determining the screening efficacy of the probe for different non-small cell lung carcinoma (NSCLC) cell lines, namely, HCC827, A549 and H1650 cells. Cell proliferation and apoptosis assays indicated that the three cell lines had different sensitivities to gefitinib. The results of analysis by living-cell fluorescence imaging and flow cytometry were consistent with those of the cell proliferation and apoptosis assays. This demonstrated that our probe could detect caspase-3 in living cells, which confirmed the apoptosis of NSCLC cells. Furthermore, our probe indicated that gefitinib was more efficient against HCC827 cells than against the other two NSCLC cell lines. This report proves that the fluorescent probe DEVD-TPE is highly sensitive to caspase-3 and has potential prospects in the rapid screening of NSCLC.
authors.affiliation: School of Chemistry and Chemical Engineering, Shanghai Key Lab of Electrical Insulation and Thermal Aging, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, P. R. China. yuesu@sjtu.edu.cn xyzhu@sjtu.edu.cn.
authors.forename: Yi
authors.initials: Y
authors.lastname: Hu
authors.affiliation: School of Chemistry and Chemical Engineering, Shanghai Key Lab of Electrical Insulation and Thermal Aging, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, P. R. China. yuesu@sjtu.edu.cn xyzhu@sjtu.edu.cn.
authors.forename: Leilei
authors.initials: L
authors.lastname: Shi
authors.affiliation: School of Chemistry and Chemical Engineering, Shanghai Key Lab of Electrical Insulation and Thermal Aging, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, P. R. China. yuesu@sjtu.edu.cn xyzhu@sjtu.edu.cn.
authors.forename: Yue
authors.identifier: http://orcid.org/0000-0002-6136-6108
authors.initials: Y
authors.lastname: Su
authors.affiliation: School of Chemistry and Chemical Engineering, Shanghai Key Lab of Electrical Insulation and Thermal Aging, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, P. R. China. yuesu@sjtu.edu.cn xyzhu@sjtu.edu.cn.
authors.forename: Chuan
authors.initials: C
authors.lastname: Zhang
authors.affiliation: School of Chemistry and Chemical Engineering, Shanghai Key Lab of Electrical Insulation and Thermal Aging, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, P. R. China. yuesu@sjtu.edu.cn xyzhu@sjtu.edu.cn.
authors.forename: Xin
authors.identifier: http://orcid.org/0000-0003-1779-6407
authors.initials: X
authors.lastname: Jin
authors.affiliation: School of Chemistry and Chemical Engineering, Shanghai Key Lab of Electrical Insulation and Thermal Aging, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, P. R. China. yuesu@sjtu.edu.cn xyzhu@sjtu.edu.cn.
authors.forename: Xinyuan
authors.identifier: http://orcid.org/0000-0002-2891-837X
authors.initials: X
authors.lastname: Zhu
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor / Q000379:methods*; D005456:Fluorescent Dyes / Q000737:chemistry*; D000077156:Gefitinib; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy*; D061848:Optical Imaging / Q000379:methods*; D010455:Peptides / Q000737:chemistry; D047428:Protein Kinase Inhibitors / Q000494:pharmacology; D011799:Quinazolines / Q000494:pharmacology*; D013267:Stilbenes / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D005456:Fluorescent Dyes; D010455:Peptides; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D013267:Stilbenes; C000617116:tetraphenylethylene; D000077156:Gefitinib