title: Color-Convertible, Unimolecular, Micelle-Based, Activatable Fluorescent Probe for Tumor-Specific Detection and Imaging In Vitro and In Vivo.
abstract: Recent years have witnessed significant progress in molecular probes for cancer diagnosis. However, the conventional molecular probes are designed to be "always-on" by attachment of tumor-targeting ligands, which limits their abilities to diagnose tumors universally due to the variations of targeting efficiency and complex environment in different cancers. Here, it is proposed that a color-convertible, activatable probe is responding to a universal tumor microenvironment for tumor-specific diagnosis without targeting ligands. Based on the significant hallmark of up-regulated hydrogen peroxide (H2O2) in various tumors, a novel unimolecular micelle constructed by boronate coupling of a hydrophobic hyperbranched poly(fluorene-co-2,1,3-benzothiadiazole) core and many hydrophilic poly(ethylene glycol) arms is built as an H2O2-activatable fluorescent nanoprobe to delineate tumors from normal tissues through an aggregation-enhanced fluorescence resonance energy transfer strategy. This color-convertible, activatable nanoprobe is obviously blue-fluorescent in various normal cells, but becomes highly green-emissive in various cancer cells. After intravenous injection to tumor-bearing mice, green fluorescent signals are only detected in tumor tissue. These observations are further confirmed by direct in vivo and ex vivo tumor imaging and immunofluorescence analysis. Such a facile and simple methodology without targeting ligands for tumor-specific detection and imaging is worthwhile to further development.
authors.affiliation: School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Huang
authors.affiliation: School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai, 201418, China.
authors.forename: Feng
authors.initials: F
authors.lastname: Qiu
authors.affiliation: School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, China.
authors.forename: Dong
authors.initials: D
authors.lastname: Chen
authors.affiliation: Department of Oral Maxillofacial-Head Neck Oncology, Ninth People's Hospital, Shanghai Jiao Tong University, 639 Zhizaoju Road, Shanghai, 200011, China.
authors.forename: Lingyue
authors.initials: L
authors.lastname: Shen
authors.affiliation: School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, China.
authors.forename: Shuting
authors.initials: S
authors.lastname: Xu
authors.affiliation: School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, China.
authors.forename: Dongbo
authors.initials: D
authors.lastname: Guo
authors.affiliation: School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, China.
authors.forename: Yue
authors.initials: Y
authors.lastname: Su
authors.affiliation: School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, China.
authors.forename: Deyue
authors.initials: D
authors.lastname: Yan
authors.affiliation: School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, China.
authors.forename: Xinyuan
authors.initials: X
authors.lastname: Zhu
mesh_terms: D000818:Animals; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D003116:Color; D003952:Diagnostic Imaging / Q000379:methods*; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D008823:Micelles; D009369:Neoplasms / Q000000981:diagnostic imaging*; D009928:Organ Specificity; D011092:Polyethylene Glycols / Q000737:chemistry; D013050:Spectrometry, Fluorescence; D013056:Spectrophotometry, Ultraviolet; D014018:Tissue Distribution
chemical_list: D052160:Benzothiazoles; D005456:Fluorescent Dyes; D008823:Micelles; D011092:Polyethylene Glycols
keywords: activatable probes; cancer diagnosis; color-conversion; conjugated polymers; unimolecular micelles