Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372537 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
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 °C.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Nicholas J. Baumhover, Molly E. Martin, Sharavathi G. Parameswarappa, Kyle C. Kloepping, M. Sue O’Dorisio, F. Christopher Pigge, Michael K. Schultz,