Approaching 'Kit-Type' Labelling with (68)Ga: The DATA Chelators

ChemMedChem. 2015 Jun;10(6):1019-26. doi: 10.1002/cmdc.201500092. Epub 2015 Apr 21.

Abstract

The DATA chelators are a novel class of tri-anionic ligands based on 6-amino-1,4-diazepine-triacetic acid, which have been introduced recently for the chelation of (68)Ga. Compared with macrocyclic chelators based on the cyclen scaffold (i.e., DOTA, DO3A, and DO2A derivatives), DATA chelators undergo quantitative radiolabelling more rapidly and under milder conditions. In this study, a systematic evaluation of the labelling of four DATA chelators--DATA(M), DATA(P), DATA(Ph), and DATA(PPh)--with (68)Ga is presented. The results highlight the extraordinary potential of this new class of chelators for application in molecular imaging using (68)Ga positron emission tomography (PET).

Keywords: chelates; gallium-68; ligand design; macrocyclic ligands; radiopharmaceuticals.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chelating Agents / chemistry*
  • Gallium Radioisotopes / chemistry*
  • Isotope Labeling
  • Kinetics

Substances

  • Chelating Agents
  • Gallium Radioisotopes