Current State of Targeted Radiometal-Based Constructs for the Detection and Treatment of Disease in the Brain
- Bioconjug Chem. 2021 Jul 21;32(7):1331-1347. doi: 10.1021/acs.bioconjchem.1c00180.
- 1. Ph.D. Program in Chemistry, Graduate Center of the City University of New York, New York, New York 10016, United States.
- 2. Department of Chemistry, Lehman College of the City University of New York, New York, New York 10468, United States.
- 3. Department of Chemistry, Hunter College of the City University of New York, New York, New York 10065, United States.
- 4. Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.
- 5. Collider Accelerator Department, Brookhaven National Laboratory, Upton, New York 11973, United States.
The continual development of radiopharmaceutical agents for the field of nuclear medicine is integral to promoting the necessity of personalized medicine. One way to greatly expand the selection of radiopharmaceuticals available is to broaden the range of radionuclides employed in such agents. Widening the scope of development to include radiometals with their variety of physical decay characteristics and chemical properties opens up a myriad of possibilities for new actively targeted molecules and bioconjugates. This is especially true to further advance the imaging and treatment of disease in the brain. Over the past few decades, imaging of disease in the brain has heavily relied on agents which exploit metabolic uptake. However, through utilizing the broad range of physical characteristics that radiometals offer, the ability to target Other processes has become more available. The varied chemistries of radiometals also allows for them to incorporated into specifically designed diverse constructs. A major limitation to efficient treatment of disease in the brain is the ability for relevant agents to penetrate the blood-brain barrier. Thus, along with efficient disease targeting, there must be intentional thought put into overcoming this challenge. Here, we review the current field of radiometal-based agents aimed at either imaging or therapy of brain disease that have been evaluated through at least in vivo studies.