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Cathepsin B‐Specific Metabolic Precursor for In Vivo Tumor‐Specific Fluorescence Imaging |
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| Authors: | Man Kyu Shim Dr Hong Yeol Yoon Dr Ju Hee Ryu Dr Heebeom Koo Dr Sangmin Lee Dr Jae Hyung Park Dr Jong‐Ho Kim Dr Seulki Lee Dr Martin G Pomper Dr Ick Chan Kwon Dr Kwangmeyung Kim |
| Institution: | 1. Center for Theragnosis, Biomedical Research Institute, Korea Institute of Science and Technology, Seongbuk-gu, Seoul, Republic of Korea;2. Department of Pharmacy, Graduate School, Kyung Hee University, Dongdaemun-gu, Seoul, Republic of Korea;3. School of Chemical Engineering, Sungkyunkwan University, Jangan-gu, Suwon, Republic of Korea;4. Department of Medical Life Science, College of Medicine, The Catholic University of Korea, Seocho-gu, Seoul, Republic of Korea;5. The Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University School of Medicine, Baltimore, MD, USA;6. KU-KIST Graduate School of Converging Science and Technology, Korea University, Seongbuk-gu, Seoul, Republic of Korea |
| 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. |
| Keywords: | click chemistry drug delivery imaging agents metabolic glycoengineering tumor targeting |