期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 19, 页码 5757-5761出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.08.017
关键词
Copper free click chemistry; Cyclooctyne; Peptide synthesis; Gallium-68; Copper-64; Melanocyte stimulating hormone; Molecular imaging; PET; Radionuclide therapy; PRRT
资金
- University of Iowa Holden Comprehensive Cancer Center
- American Cancer Society [IRG-77004-31]
- Roy J. Carver Charitable Trust [RJCCT 01-224, 09-3279]
- Direct For Mathematical & Physical Scien
- Division Of Chemistry [0946779] Funding Source: National Science Foundation
Radionuclide chelators (DOTA, NOTA) functionalized with a monofluorocyclooctyne group were prepared. These materials reacted rapidly and in high yield with a fully deprotected azide-modified peptide via Cu-free click chemistry under mild reaction conditions (aqueous solution, room temperature). The resulting bioconjugates bind with high affinity and specificity to their cell-surface receptor targets in vitro and appear stable to degradation in mouse serum over 3 h of incubation at 37 degrees C. (C) 2011 Elsevier Ltd. All rights reserved.
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