Amyloid-ß probes: Review of structure-activity and brain-kinetics relationships

Todd J. Eckroat, Abdelrahman S. Mayhoub, Sylvie Garneau-Tsodikova

Research output: Contribution to journalReview article

26 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)1012-1044
Number of pages33
JournalBeilstein Journal of Organic Chemistry
Volume9
DOIs
StatePublished - May 28 2013

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Amyloid
Brain
Kinetics
Monitoring

All Science Journal Classification (ASJC) codes

  • Organic Chemistry

Cite this

Eckroat, Todd J. ; Mayhoub, Abdelrahman S. ; Garneau-Tsodikova, Sylvie. / Amyloid-ß probes : Review of structure-activity and brain-kinetics relationships. In: Beilstein Journal of Organic Chemistry. 2013 ; Vol. 9. pp. 1012-1044.
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Amyloid-ß probes : Review of structure-activity and brain-kinetics relationships. / Eckroat, Todd J.; Mayhoub, Abdelrahman S.; Garneau-Tsodikova, Sylvie.

In: Beilstein Journal of Organic Chemistry, Vol. 9, 28.05.2013, p. 1012-1044.

Research output: Contribution to journalReview article

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AB - 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.

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