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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Grand Ballroom |
| Time |
10월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-302 |
| Subject |
Development of novel Quinoline Derivatives for a Fluorescent Imaging Probe with Binding Selectivity to tau |
| Authors |
Wonhee Jung, Taek Kang1, Nakcheol Jeong, Gyo chang Keum2,*
Department of Chemistry, Korea University, Korea
1Korea Institute of Science and Technology, Korea
2Chemoinformatics Research Center, Korea Institute of Science and Technology, Korea
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| Abstract |
Alzheimer’s disease (AD) is one of the chronic neurodegenerative disease and the most common cause of dementia. Post-mortem studies of AD brains have revealed two pathological hallmarks of the disease. The first one is extracellular amyloid beta (Aβ) plaques which affect the interaction between neuronal process at synapse. And the second is intracellular neurofibrillary tangles (NFTs) formed by tau protein, also disrupt on synaptic function. Tau proteins stabilize microtubules in neurons. By abnormal mutation or hyper-phosphorylation, tau proteins separated from microtubules. Separated tau proteins form insoluble PHF-tau (paired helical filament) and NFTs by self-aggregation. In the recent research, the density of Aβ plaques doesn’t correlate well with the progress of neurodegeneration or cognitive impairment in AD. In contrast, the density and neocortical spread degree of NFTs correlate well with progressive neuronal degeneration and cognitive decline in AD patients. Thus NFTs are the desirable biomarker for AD and the binding selectivity to tau over Aβ is needed to develop a probe for diagnosis the AD. It is reported that some quinoline moieties are specifically targeting tau aggregates. In this research, we designed and synthesized the quinoline derivatives that is 2,6-disubstituted by electron withdrawing groups or electron donating groups based on the donor-π-acceptor architecture for developing the fluorescent imaging probe that has selectivity to tau over Aβ. The result of in vitro studies about selectivity and fluorescence intensity will be presented in detail. |
| E-mail |
whas35@kist.re.kr |
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122nd General Meeting of the KCS