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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-293 |
| Subject |
Synthesis and Biological Evaluation of Novel Tau Aggregation Inhibitors for the Treatment of Alzheimer’s Disease |
| Authors |
Dami Lim, Ae Nim Pae1,*, Sang Min Lim1, Jae Yeol Lee2
Department of KHU-KIST Converging Science and Technology, Kyung Hee University, Korea
1Korea Institute of Science and Technology, Korea
2Department of Chemistry, Kyung Hee University, Korea
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| Abstract |
Alzheimer’s disease (AD) is a neurodegenerative disease and the most common cause for dementia. With the advent of an aging society, the importance of Alzheimer's disease is increasing. However, there is currently no treatment options that can completely cure AD. Neurofibrillary tangles (NFTs) are one of the main hallmarks of AD and primarily composed of tau protein. In the AD patient’s brain, tau protein, which stabilizes microtubules is hyperphosphorylated and then self-aggregates to form NFTs. NFTs induce neuronal damage resulting in diseases like AD. We envisaged that inhibition of the formation of NFTs would be beneficial for the treatment of AD, and therefore we are developing tau aggregation inhibitors.
Through screening based on tau-BiFC (bimolecular fluorescence complementation) assay with in-house and commercially available compound libraries, we found promising hit compounds. They showed excellent tau aggregation inhibitory activity, but some of their drug-like properties need to be improved to be AD drug candidates. Therefore, we are optimizing hit compounds to further increase potency and drug-like properties, including BBB (brain-blood barrier) penetration. |
| E-mail |
t17054@kist.re.kr |
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122nd General Meeting of the KCS