Nucl Med Mol Imaging.  2018 Feb;52(1):24-30. 10.1007/s13139-017-0484-7.

Development of tau PET Imaging Ligands and their Utility in Preclinical and Clinical Studies

Affiliations
  • 1Department of Nuclear Medicine, College of Medicine, Seoul National University, 110-744, 28 Yongon-Dong, Jongno-Gu, Seoul, South Korea. dsl@plaza.snu.ac.kr
  • 2Department of Nuclear Medicine, Seoul National University Hospital, 28Yongon-Dong, Jongno-Gu, Seoul 110-744, South Korea.
  • 3Department of MolecularMedicine and Biopharmaceutical Sciences, Graduate School of Convergence Science and Technology, and College of Medicine or College of Pharmacy, Seoul National University, 03080, 103 Daehak-ro, Jongno-gu, Seoul, South Korea.
  • 4Institute of Brain Science, Korean Institute of Science and Technology, Hwarangno 14-gil 5, Seongbuk-gu, Seoul 136-791, South Korea. djk2991@kist.re.kr

Abstract

The pathological features of Alzheimer's disease are senile plaques which are aggregates of β-amyloid peptides and neurofibrillary tangles in the brain. Neurofibrillary tangles are aggregates of hyperphosphorylated tau proteins, and these induce various other neurodegenerative diseases, such as progressive supranuclear palsy, corticobasal degeneration, frontotemporal lobar degeneration, frontotemporal dementia and parkinsonism linked to chromosome 17 (FTDP-17), and chronic traumatic encephalopathy. In the case of Alzheimer's disease, the measurement of neurofibrillary tangles associated with cognitive decline is suitable for differential diagnosis, disease progression assessment, and to monitor the effects of therapeutic treatment. This review discusses considerations for the development of tau ligands for imaging and summarizes the results of the first-in-human and preclinical studies of the tau tracers that have been developed thus far. The development of tau ligands for imaging studies will be helpful for differential diagnosis and for the development of therapeutic treatments for tauopathies including Alzheimer's disease.

Keyword

Tau; Alzheimer's disease; Tauopathy; Pet; Imaging ligands; Radiopharmaceutical

MeSH Terms

Alzheimer Disease
Brain
Brain Injury, Chronic
Chromosomes, Human, Pair 17
Diagnosis, Differential
Disease Progression
Frontotemporal Dementia
Frontotemporal Lobar Degeneration
Ligands*
Neurodegenerative Diseases
Neurofibrillary Tangles
Parkinsonian Disorders
Peptides
Plaque, Amyloid
Supranuclear Palsy, Progressive
tau Proteins
Tauopathies
Ligands
Peptides
tau Proteins
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