title: Amyloid-β probes: Review of structure-activity and brain-kinetics relationships.
abstract: The number of people suffering from Alzheimer's disease (AD) is expected to increase dramatically in the coming years, placing a huge burden on society. Current treatments for AD leave much to be desired, and numerous research efforts around the globe are focused on developing improved therapeutics. In addition, current diagnostic tools for AD rely largely on subjective cognitive assessment rather than on identification of pathophysiological changes associated with disease onset and progression. These facts have led to numerous efforts to develop chemical probes to detect pathophysiological hallmarks of AD, such as amyloid-β plaques, for diagnosis and monitoring of therapeutic efficacy. This review provides a survey of chemical probes developed to date for AD with emphasis on synthetic methodologies and structure-activity relationships with regards to affinity for target and brain kinetics. Several probes discussed herein show particularly promising results and will be of immense value moving forward in the fight against AD.
authors.affiliation: Department of Pharmaceutical Sciences, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, United States ; Life Sciences Institute and Department of Medicinal Chemistry, University of Michigan, 210 Washtenaw Ave, Ann Arbor, MI, 48109-2216, United States.
authors.forename: Todd J
authors.initials: TJ
authors.lastname: Eckroat
authors.forename: Abdelrahman S
authors.initials: AS
authors.lastname: Mayhoub
authors.forename: Sylvie
authors.initials: S
authors.lastname: Garneau-Tsodikova
keywords: Alzheimer’s disease; PET/SPECT imaging; in vivo detection; near-infrared fluorescence probes; radioactive probes