Radioactive Main Group and Rare Earth Metals for Imaging and Therapy
Top Cited Papers
- 31 October 2018
- journal article
- review article
- Published by American Chemical Society (ACS) in Chemical Reviews
- Vol. 119 (2), 902-956
- https://doi.org/10.1021/acs.chemrev.8b00294
Abstract
Radiometals possess an exceptional breadth of decay properties and have been applied to medicine with great success for several decades. The majority of current clinical use involves diagnostic procedures, which use either positron-emission tomography (PET) or single-photon imaging to detect anatomic abnormalities that are difficult to visualize using conventional imaging techniques (e.g., MRI and X-ray). The potential of therapeutic radiometals has more recently been realized and relies on ionizing radiation to induce irreversible DNA damage, resulting in cell death. In both cases, radiopharmaceutical development has been largely geared toward the field of oncology; thus, selective tumor targeting is often essential for efficacious drug use. To this end, the rational design of four-component radiopharmaceuticals has become popularized. This Review introduces fundamental concepts of drug design and applications, with particular emphasis on bifunctional chelators (BFCs), which ensure secure consolidation of the radiometal and targeting vector and are integral for optimal drug performance. Also presented are detailed accounts of production, chelation chemistry, and biological use of selected main group and rare earth radiometals.Funding Information
- Canadian Institutes of Health Research
- Natural Sciences and Engineering Research Council of Canada
- University of British Columbia
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