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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-286 |
| Subject |
Studies on the discovery of Novel Tau Aggregation Inhibitors for the Treatment of Alzheimer’s Disease
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| Authors |
HyoJin Kim, HyeanJeong Jeong1, Yun Kyung Kim2, Ae Nim Pae2, Cheol-Hong Cheon*, Sang Min Lim2,*
Department of Chemistry, Korea University, Korea
1Korea University, Korea
2Korea Institute of Science and Technology, Korea
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| Abstract |
Alzheimer's disease (AD) is one of the most common neurodegenerative diseases that must be studied because it becomes a serious problem in an aging society. Although AD has been extensively studied, there are only drugs that alleviate some of the symptoms of Alzheimer's disease, and there are no disease-modifying drugs. Tau is a microtubule associated protein (MAP) that binds to and stabilizes microtubules. However, hyperphosphorylation of tau induces the separation from the microtubules, and the separated tau self-assembles forming tau oligomers and aggregates that result in induction of neuronal loss and eventually neurodegenerative diseases such as AD. Therefore, we develop tau aggregation inhibitors to find drug candidates for the treatment of AD. To discover new hit compounds that can inhibit tau aggregation, we performed a high-throughput screening based on Bi-FC assay with in-house compound libraries. By modifying hit compounds, we have found compounds that are more potent and less toxic than Methylene blue: a well-known in vitro tau aggregation inhibitor. Currently, a variety of derivatives have been synthesized through a structure-activity relationship study to find compounds that are more potent than the hit compounds. We will continue to work to further optimize potency as well as physicochemical properties to develop clinical candidates. |
| E-mail |
t16895@kist.re.kr |
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122nd General Meeting of the KCS