title: Current advances in ligand design for inorganic positron emission tomography tracers68Ga,64Cu,89Zr and44Sc.
abstract: A key part of the development of metal based Positron Emission Tomography probes is the chelation of the radiometal. In this review the recent developments in the chelation of four positron emitting radiometals,68Ga,64Cu,89Zr and44Sc, are explored. The factors that effect the chelation of each radio metal and the ideal ligand system will be discussed with regards to high in vivo stability, complexation conditions, conjugation to targeting motifs and complexation kinetics. A series of cyclic, cross-bridged and acyclic ligands will be discussed, such as CP256 which forms stable complexes with68Ga under mild conditions and PCB-TE2A which has been shown to form a highly stable complex with64Cu.89Zr and44Sc have seen significant development in recent years with a number of chelates being applied to each metal - eight coordinate di-macrocyclic terephthalamide ligands were found to rapidly produce more stable complexes with89Zr than the widely used DFO.
authors: School of Biological, Biomedical and Environmental Sciences, The University of Hull, HU6 7RX, UK. g.stasiuk@hull.ac.uk and Positron Emission Tomography Research Centre, The University of Hull, HU6 7RX, UK.
authors: Thomas W
authors: TW
authors: Price
authors: School of Biological, Biomedical and Environmental Sciences, The University of Hull, HU6 7RX, UK. g.stasiuk@hull.ac.uk.
authors: John
authors: J
authors: Greenman
authors: School of Biological, Biomedical and Environmental Sciences, The University of Hull, HU6 7RX, UK. g.stasiuk@hull.ac.uk and Positron Emission Tomography Research Centre, The University of Hull, HU6 7RX, UK.
authors: Graeme J
authors: GJ
authors: Stasiuk