Price Thomas W, Greenman John, Stasiuk Graeme J
School of Biological, Biomedical and Environmental Sciences, The University of Hull, HU6 7RX, UK.
Dalton Trans. 2016 Oct 12;45(40):15702-15724. doi: 10.1039/c5dt04706d.
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, Ga, Cu, Zr and Sc, 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 with Ga under mild conditions and PCB-TE2A which has been shown to form a highly stable complex with Cu. Zr and Sc 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 with Zr than the widely used DFO.
金属基正电子发射断层扫描探针开发的一个关键部分是放射性金属的螯合。在这篇综述中，探讨了四种正电子发射放射性金属（镓、铜、锆和钪）螯合方面的最新进展。将讨论影响每种放射性金属螯合的因素以及理想的配体系统，涉及体内高稳定性、络合条件、与靶向基序的共轭以及络合动力学。将讨论一系列环状、交叉桥连和非环状配体，例如在温和条件下与镓形成稳定络合物的CP256以及已证明与铜形成高度稳定络合物的PCB-TE2A。近年来，锆和钪有了显著进展，许多螯合物被应用于每种金属——发现八配位双大环对苯二甲酰胺配体与锆形成的络合物比广泛使用的去铁胺更快且更稳定。
