title: An intracellularly activatable, fluorogenic probe for cancer imaging.
abstract: A newly designed, dual-functional probe based on intracellular activation has been successfully developed for the detection of cancer cells. The probe is nearly non-fluorescent in buffer due to its highly efficient FRET quenching, but it can be specifically activated with dramatic fluorescence enhancement upon intracellular cathepsin B cleavage in target cancer cells after selective internalization via folate receptor-dependent endocytosis. Therefore, this probe enables "turn-on" visualization of cancer cells with desirable specificity and contrast enhancement. This targeted, intracellularly activatable probe exhibits low fluorescence-quenched background when compared with "always-on" probes and avoids non-specific activation by non-specifically expressed enzymes in normal tissue, which normally occurs when using common "turn on" probe design strategies. Therefore, this probe can be potentially applied in intraoperative inspection during clinical cancer surgery with higher contrast and sensitivity.
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin 300071, P. R. China. hongzy@nankai.edu.cn.
authors.forename: Ruisong
authors.initials: R
authors.lastname: Tian
authors.forename: Mingjie
authors.initials: M
authors.lastname: Li
authors.forename: Jin
authors.initials: J
authors.lastname: Wang
authors.forename: Min
authors.initials: M
authors.lastname: Yu
authors.forename: Xiuqi
authors.initials: X
authors.lastname: Kong
authors.forename: Yupeng
authors.initials: Y
authors.lastname: Feng
authors.forename: Zeming
authors.initials: Z
authors.lastname: Chen
authors.forename: Yuxi
authors.initials: Y
authors.lastname: Li
authors.forename: Weiqiang
authors.initials: W
authors.lastname: Huang
authors.forename: Wenjie
authors.initials: W
authors.lastname: Wu
authors.forename: Zhangyong
authors.initials: Z
authors.lastname: Hong
mesh_terms: D000818:Animals; D002401:Cathepsin B; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D005434:Flow Cytometry; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry; D005492:Folic Acid / Q000378:metabolism; D006801:Humans; D042541:Intracellular Space / Q000378:metabolism*; D051379:Mice; D018613:Microscopy, Confocal; D057054:Molecular Imaging / Q000379:methods*; D041681:NIH 3T3 Cells; D009369:Neoplasms / Q000175:diagnosis* / Q000473:pathology; D010949:Plasma / Q000378:metabolism; D015203:Reproducibility of Results; D013050:Spectrometry, Fluorescence; D013056:Spectrophotometry, Ultraviolet; D013696:Temperature; D013997:Time Factors
chemical_list: D005456:Fluorescent Dyes; D005492:Folic Acid; D002401:Cathepsin B