Shim, Man Kyu Yoon, Hong Yeol Lee, Sangmin Jo, Mun Kyeong Park, Jooho Kim, Jong-Ho Jeong, Seo Young Kwon, Ick Chan Kim, Kwangmeyung 2024-01-20T00:02:45Z 2024-01-20T00:02:45Z 2021-09-03 2017-11-30 2045-2322 https://pubs.kist.re.kr/handle/201004/122034 Apoptosis is one of the most important intracellular events in living cell, which is a programmed cell death interrelated with caspase enzyme activity for maintaining homeostasis in multicellular organisms. Therefore, direct apoptosis imaging of living cells can provide enormous advantages for diagnosis, drug discovery, and therapeutic monitoring in various diseases. However, a method of direct apoptosis imaging has not been fully validated, especially for live cells in in vitro and in vivo. Herein, we developed a new apoptosis imaging technology via a direct visualization of active caspase-3/-7 activity in living cells. For this, we synthesized a caspase-3/-7-specific cleavable peptide (KGDEVD) conjugated triacetylated N-azidoacetyl-D-mannosamine (Apo-S-Ac(3)ManNAz), wherein the Apo-S-Ac(3)ManNAz can be cleaved by the active caspase-3/-7 in live apoptotic cells and the cleaved Ac(3)ManNAz molecules can further generate targetable azido groups (N-3) on the living cell surface. Importantly, the azido groups on the apoptotic tumor cells could be visualized with Cy5.5-conjugated dibenzylcyclooctyne (DBCO-Cy5.5) via bioorthogonal click chemistry in vitro cell culture condition and in vivo tumor-bearing mice. Therefore, our Apo-S-Ac(3)ManNAz can be utilized for the further applications in tumor therapy as a monitoring tool for anticancer efficacy and optimization of anticancer new drugs in cell culture system and in tumor-bearing mice. English NATURE PUBLISHING GROUP IN-VIVO CATHEPSIN-B NECROSIS-FACTOR CELL APOPTOSIS ANNEXIN-V FLUORESCENT DISEASE NANOPARTICLES EXPRESSION INHIBITORS Caspase-3/-7-Specific Metabolic Precursor for Bioorthogonal Tracking of Tumor Apoptosis Article 10.1038/s41598-017-16653-2 1 SCIENTIFIC REPORTS, v.7 SCIENTIFIC REPORTS 7 scie scopus 000416891400037 2-s2.0-85037052666 Multidisciplinary Sciences Science & Technology - Other Topics Article IN-VIVO CATHEPSIN-B NECROSIS-FACTOR CELL APOPTOSIS ANNEXIN-V FLUORESCENT DISEASE NANOPARTICLES EXPRESSION INHIBITORS