Solid-Supported NOTA and DOTA Chelators Useful for the Synthesis of 3 '-Radiometalated Oligonucleotides



: Kiviniemi A, Makela J, Makila J, Saanijoki T, Liljenback H, Poijarvi-Virta P, Lonnberg H, Laitala-Leinonen T, Roivainen A, Virta P

Publisher: AMER CHEMICAL SOC

: 2012

: Bioconjugate Chemistry

: BIOCONJUGATE CHEMISTRY

: BIOCONJUGATE CHEM

: 9

: 23

: 9

: 1981

: 1988

: 8

: 1043-1802

DOI: https://doi.org/10.1021/bc300253t(external)


Esterified precursors of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA; 18) and 1,4,7-triazacyclononane-1,4,7-trisacetic acid (NOTA; 17,19) ligands bearing a dimethoxytritylated hydroxyl side arm were prepared and immobilized via an ester linkage to long chain alkyl amine derivatized controlled pore glass (LCAA-CPG). Oligonucleotide chains were then assembled on the hydroxyl function and conjugates were released and deprotected by a two-step cleavage with aqueous alkali and ammonia. The 3'-DOTA and 3'-NOTA conjugated oligonucleotides were converted to Ga-68 chelates by a brief treatment with [Ga-68]Cl-3 at elevated temperature. Applicability of the conjugates for in vivo imaging with positron emission tomography (PET) was verified.



Last updated on 2024-26-11 at 22:22