4.7 Review

Recent development in selective Tau tracers for PET imaging in the brain

Journal

CHINESE CHEMICAL LETTERS
Volume 33, Issue 7, Pages 3339-3348

Publisher

ELSEVIER SCIENCE INC
DOI: 10.1016/j.cclet.2022.03.024

Keywords

Tau; PET imaging; Tauopathies; Alzheimer's disease; Selectivity

Funding

  1. National Natural Science Foundation of China [U1967221, 22022601]

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This review summarizes the latest development of Tau tracers and analyzes their chemical structures and biological properties. The limitations of current tracers and considerations for the development of new tracers are also discussed.
Abnormal Tau deposition is a crucial pathological hallmark of various neurodegenerative disorders defined as tauopathies, of which Alzheimer's disease is the most prominent one. To date, a large number of chemical entities with different structures have been developed as Tau imaging tracers for the early diagnosis of tauopathies. Several of them with excellent bio-properties are currently being assessed in clinical trials, and more recently, the Tauvid (TM) ([(18) F]Flortaucipir, also known as [F-18]AV1451 or [F-18]T807) as the first Tau tracer was approved by the U.S. Food and Drug Administration in 2020. This review summarized the latest development of Tau tracers and analyzed their chemical structures, with particular attention to the effects of chemical structures on biological properties. In addition, we also discuss the limitations of current Tau imaging tracers, issues that need attention in the development of new tracers, and possible future directions. (C) 2022 Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.

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