Solid-supported NOTA and DOTA chelators useful for the synthesis of 3'-radiometalated oligonucleotides

Bioconjug Chem. 2012 Sep 19;23(9):1981-8. doi: 10.1021/bc300253t. Epub 2012 Aug 20.

Abstract

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 (68)Ga chelates by a brief treatment with [(68)Ga]Cl(3) at elevated temperature. Applicability of the conjugates for in vivo imaging with positron emission tomography (PET) was verified.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chelating Agents / chemistry*
  • Magnetic Resonance Spectroscopy
  • Oligonucleotides / chemistry*
  • Positron-Emission Tomography
  • Spectrometry, Mass, Electrospray Ionization

Substances

  • Chelating Agents
  • Oligonucleotides