DOTA and its derivatives are most widely used novel bifunctional chelators. They have not only mature synthesis route, but also good coordination and chelating ability. Therefore, DOTA metal complexes of DOTA-peptide conjugates are increasingly used as MRI contrast agents, radionuclide targeted imaging agents and therapeutic radiopharmaceuticals in the biomedical field. This review covers the bifunctional derivatives of DOTA, the synthesis of DOTA-peptide conjugates, and the applications of DOTA-peptide conjugate metal complexes.

DOTA; Analogs & derivatives; Isotope labeling; Metals; Trends