title: Real-Time Specific Light-Up Sensing of Transferrin Receptor: Image-Guided Photodynamic Ablation of Cancer Cells through Controlled Cytomembrane Disintegration.
abstract: Transferrin receptor (TfR) represents a unique target for specific imaging of cancer cells and targeted delivery of therapeutic reagents. Detection and qualification of TfR is thus of great importance for cancer diagnosis and therapy. In this contribution, a light-up probe TPETH-2T7 was developed by conjugating a red-emissive photosensitizer with aggregation-induced emission (AIE) characteristics to a TfR-targeting peptide T7. The probe is almost nonemissive by itself, but it gives turn-on fluorescence in the presence of TfR with a detection limit of 0.45 μg/mL. Cellular experiments show that the probe specifically binds to TfR-overexpressed cancer cells. Real-time imaging results reveal that the probe stains the MDA-MB-231 cell membrane in 30 min, which is followed by probe internalization. Experiments on image-guided photodynamic cancer ablation show that the therapeutic performance is better when TPETH-2T7 is localized on the cell membrane as compared to that being internalized into cells. Confocal laser scanning microscopy (CLSM) study reveals that cytomembrane disintegration allows quick ablation of MDA-MB-231 cells.
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore , 4 Engineering Drive 4, Singapore 117585.
authors.forename: Ruoyu
authors.initials: R
authors.lastname: Zhang
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore , 4 Engineering Drive 4, Singapore 117585.
authors.forename: Guangxue
authors.initials: G
authors.lastname: Feng
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore , 4 Engineering Drive 4, Singapore 117585.
authors.forename: Chong-Jing
authors.initials: CJ
authors.lastname: Zhang
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore , 4 Engineering Drive 4, Singapore 117585.
authors.forename: Xiaolei
authors.initials: X
authors.lastname: Cai
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore , 4 Engineering Drive 4, Singapore 117585.
authors.forename: Xiamin
authors.initials: X
authors.lastname: Cheng
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore , 4 Engineering Drive 4, Singapore 117585.|Institute of Materials Research and Engineering (Astar) , 3 Research Link, Singapore 117602.
authors.forename: Bin
authors.initials: B
authors.lastname: Liu
mesh_terms: D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D002462:Cell Membrane / Q000737:chemistry / Q000378:metabolism*; D002470:Cell Survival / Q000187:drug effects; D005260:Female; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D008027:Light; D018613:Microscopy, Confocal; D015394:Molecular Structure; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000737:chemistry / Q000494:pharmacology*; D011990:Receptors, Transferrin / Q000032:analysis* / Q000096:biosynthesis; D013997:Time Factors; D014407:Tumor Cells, Cultured
chemical_list: D005456:Fluorescent Dyes; D017319:Photosensitizing Agents; D011990:Receptors, Transferrin