RESUMO
Radiolabeled biomolecules with short half-life times are of increasing importance for positron emission tomography (PET) imaging studies. Herein, we demonstrate an improved and generalized method for synthesizing a [radiometal]-unsaturated aldehyde as a lysine-labeling probe that can be easily conjugated into various biomolecules through the RIKEN click reaction. As a case study, 68 Ga-PET imaging of U87MG xenografted mice is demonstrated by using the 68 Ga-DOTA-RGDyK peptide, which is selective to αV ß3 integrins.
Assuntos
Radioisótopos de Gálio/farmacocinética , Peptídeos/farmacocinética , Tomografia por Emissão de Pósitrons/métodos , Compostos Radiofarmacêuticos/farmacocinética , Animais , Linhagem Celular Tumoral , Radioisótopos de Gálio/química , Xenoenxertos , Humanos , Integrina alfaVbeta3/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Peptídeos/química , Distribuição TecidualRESUMO
The unsaturated ester aldehyde, (E)-3-alkoxycarbonyl-5-phenyl-2,4-dienal, was efficiently dimerized by applying the strain-promoted double-click reaction with sym-dibenzo-1,5-cyclooctadiene-3,7-diyne. The resulting dimerized probe was sequentially reacted first with one peptide molecule and then with a protein or the amino groups on the surface of a live cell through double azaelectrocyclization to achieve highly efficient bioconjugation.
Assuntos
Aldeídos/química , Alcinos/química , Animais , Sobrevivência Celular , Ciclização , Dimerização , Ésteres , Células HeLa , Humanos , Camundongos , Peptídeos/química , Albumina Sérica/químicaRESUMO
Versatile method for living cell labeling has been established. Cell surfaces are initially biotinylated by azaelectrocyclization, and then treated with the fluorescence-labeled avidin or the anti-biotin antibody.
