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Photosensitizer-conjugated tryptophan-containing peptide ligands as new dual-targeted theranostics for cancers

Title
Photosensitizer-conjugated tryptophan-containing peptide ligands as new dual-targeted theranostics for cancers
Authors
Kim J.Chae J.Kim J.S.Goh S.-H.Choi Y.
Ewha Authors
김준수
SCOPUS Author ID
김준수scopus
Issue Date
2016
Journal Title
International Journal of Pharmaceutics
ISSN
0378-5173JCR Link
Citation
vol. 513, no. 42737.0, pp. 584 - 590
Keywords
ActivatableEGFR targetFluorescence imagingPhotodynamic therapyTheranostics
Publisher
Elsevier
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Here we report that new dual-targeted theranostic anti-cancer agents can be produced by simple conjugation of photosensitizers with tryptophan-containing peptide ligands via cyclic disulfide linkages. In the proof-of-concept study, photosensitizers conjugated with EGFR-targeting peptide GE11 (C-EGFR) were in close proximity with tryptophan residues in the conjugate, resulting in quenching of its fluorescence and singlet oxygen generation. C-EGFR specifically binds to target receptors on the cancer cell surface, after which it is internalized via receptor-mediated endocytosis. Intracellular cleavage of cyclic disulfide bonds allows separation of the photosensitizers from the tryptophan residue, after which they emit near-infrared (NIR) fluorescence and produce a phototoxic effect in the target cells. This strategy enabled us to accomplish simultaneous real-time NIR fluorescence imaging of EGFR-overexpressing cancer cells with high contrast and selective photodynamic therapy © 2016 Elsevier B.V.
DOI
10.1016/j.ijpharm.2016.09.071
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자연과학대학 > 화학·나노과학전공 > Journal papers
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