IEDDA Conjugation Reaction in Radiometal Labeling of Peptides with ⁶⁸Ga and ⁶⁴Cu: Unexpected Findings.

ABSTRACT: The inverse electron demand Diels-Alder conjugation reaction has gained increasing importance over the past few years for efficient in vivo and ex vivo radiometal labeling of antibodies. However, the application of this very fast reaction type has not been studied for radiolabeling of peptides so far. We show here the synthesis of 3-benzyl-1,2,4,5-tetrazine-comprising ((1,4,7,10-tetraazacyclododecane-4,7,10-triyl)triacetic acid-1-glutaric acid) (DOTA-GA) and ((1,4,7-triazacyclononane-4,7-diyl)diacetic acid-1-glutaric acid) (NODA-GA) chelators and their radiometal labeling with ⁶⁸Ga³⁺ and ⁶⁴Cu²⁺. The secondary labeling precursors ⁶⁸Ga-DOTA-GA-Tz, ⁶⁸Ga-NODA-GA-Tz, and ⁶⁴Cu-DOTA-GA-Tz were obtained in high radiochemi

SUBMITTER: Litau S 

PROVIDER: S-EPMC6217686 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature