Cathepsin B-Specific Metabolic Precursor for In Vivo Tumor-Specific Fluorescence Imaging

Title
Cathepsin B-Specific Metabolic Precursor for In Vivo Tumor-Specific Fluorescence Imaging
Authors
권익찬김광명류주희이상민윤홍열심만규구희범박재형김종호이슬기Martin G. Pomper
Keywords
click chemistry; drug delivery; imaging agents; metabolic glycoengineering; tumor targeting
Issue Date
2016-11
Publisher
Angewandte Chemie international edition
Citation
VOL 55, NO 47-14703
Abstract
Recently, metabolic glycoengineering with bioorthogonal click reactions has focused on improving the tumor targeting efficiency of nanoparticles as delivery vehicles for anticancer drugs or imaging agents. It is the key technique for developing tumor-specific metabolic precursors that can generate unnatural glycans on the tumor-cell surface. A cathepsin B-specific cleavable substrate (KGRR) conjugated with triacetylated N-azidoacetyl-d-mannosamine (RR-S-Ac3ManNAz) was developed to enable tumor cells to generate unnatural glycans that contain azide groups. The generation of azide groups on the tumor cell surface was exogenously and specifically controlled by the amount of RR-S-Ac3ManNAz that was fed to target tumor cells. Moreover, unnatural glycans on the tumor cell surface were conjugated with near infrared fluorescence (NIRF) dye-labeled molecules by a bioorthogonal click reaction in cell cultures and in tumor-bearing mice. Therefore, our RR-S-Ac3ManNAz is promising for research in tumor-specific imaging or drug delivery.
URI
http://pubs.kist.re.kr/handle/201004/64938
ISSN
1433-7851
Appears in Collections:
KIST Publication > Article
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