Recent developments in the design of bifunctional chelators for metal-based radiopharmaceuticals used in Positron Emission Tomography
- 作者：Mark D. Bartholomä ; ; mark.bartholomae@uniklinik-freiburg.de ; [Author Vitae]
- 关键词：Positron Emission Tomography ; Radiopharmaceuticals ; Bifunctional chelator ; Gallium-68 ; Copper-64
- 刊名：Inorganica Chimica Acta
- 出版年：2012
- 期刊代码：40_00201693
- 类别：ch
- 出版时间：1 July, 2012
- 卷：389
- 期：Complete
- 页码：36-51
- 文件大小：999 K
摘要
In recent years, Positron Emission Tomography (PET) has become a practical, high performance clinical imaging modality for visualization of biological process within the living system. For radiolabeling of targeting vectors, ideally determining the biological fate of the radiolabeled bioconjugate, non-traditional metal-based PET radioisotopes are of particular interest as they offer certain advantages over traditional PET radioisotopes such as longer half-lives that allow delayed imaging or availability by commercial generator systems apart from on-site cyclotron production. However, for the incorporation of the radiometal into the targeting vector, a bifunctional chelator is needed that tightly binds the radiometal at one terminus while the second terminus serves for the covalent conjugation to the biomolecule. Conjugation of a metal chelate functionality to a biovector, however, may impact the in vivo distribution of the biomolecule. This review summarizes the recent developments of bifunctional chelates for two important PET radiometals, copper-64 and gallium-68, and discusses their coordination chemistry in relation to in vivo stability and pharmacokinetics.