1227407-69-3Relevant articles and documents
Improved synthesis and biological evaluation of chelator-modified α-MSH analogs prepared by copper-free click chemistry
Baumhover, Nicholas J.,Martin, Molly E.,Parameswarappa, Sharavathi G.,Kloepping, Kyle C.,O'Dorisio, M. Sue,Pigge, F. Christopher,Schultz, Michael K.
, p. 5757 - 5761 (2011)
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.
Synthesis of a DOTA-biotin conjugate for radionuclide chelation via Cu-free click chemistry
Schultz, Michael K.,Parameswarappa, Sharavathi G.,Pigge, F. Christopher
supporting information; experimental part, p. 2398 - 2401 (2010/07/17)
A strain-induced copper-free click reaction mediated by a new and easily prepared cyclooctyne derivative was used to efficiently assemble a DOTA-biotin adduct capable of radionuclide (68Ga) uptake. This synthetic strategy offers a potentially general and convenient means of preparing targeted radiolabeling and radiotherapeutic agents.
