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Chelators are necessary in nuclear medicine imaging to direct an inorganic radionuclide, a radiometal, to a desired target; unfortunately, there is no 'one-size-fits-all' chelator. As the toolbox of radiometals is expanding, new chelators are required to prevent off-target side effects. 1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) is the current gold standard chelator for several radiometals, but typically, chelation requires harsh conditions, making it unsuitable to label biological vectors. The ideal chelator would allow labelling under mild conditions (near-neutral pH and low temperatures [∼37 °C]) and be both thermodynamically and kinetically stable. Over the past 2-3 years, several exciting chelators have been developed that have superior properties to make them worth investigating for future clinical applications.

More information Original publication

DOI

10.1016/j.cbpa.2021.03.001

Type

Journal article

Publication Date

2021-08-01T00:00:00+00:00

Volume

63

Pages

152 - 162

Total pages

10

Keywords

Lutetium-177 radiopharmaceutical, PET, Scandium-44, Zirconium-89, Animals, Chelating Agents, Coordination Complexes, Heterocyclic Compounds, 1-Ring, Humans, Hydrogen-Ion Concentration, Kinetics, Metals, Molecular Structure, Positron-Emission Tomography, Radioisotopes, Radiopharmaceuticals, Staining and Labeling, Structure-Activity Relationship, Temperature, Thermodynamics, Tomography, Emission-Computed, Single-Photon