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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Event Hall |
| Time |
4월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-587 |
| Subject |
Synthesis and Biological Evaluation of Chalcone Derivatives as Nrf2 Activator for Neurodegenerative Disease |
| Authors |
Hyeon Jeong Kim, Ki Duk Park*
Convergence Research Center for DTC, Korea Institute of Science and Technology, Korea
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| Abstract |
Neurodegenerative disease is characterized by progressive degeneration and death of neurons, resulting in neural network dysfunction. As the underlying mechanisms, it has been reported that oxidative damage can lead to neuronal toxicity and finally neuronal cell death. Nrf2-ARE signaling pathway has been well-known as a primary cellular defense mechanism against oxidative damage. Under oxidative or inflammatory stressed conditions, Nrf2, a transcription factor, regulates the cellular redox balance by inducing expression of antioxidant enzyme genes. In this study, we have synthesized novel chalcone derivatives as Nrf2 activators. Among the derivatives, KDS3021 showed significant efficacy for activating Nrf2 and induced expression of the Nrf2 dependent antioxidant enzymes such as HO-1, GCLM and NQO1. In addition, KDS3021 effectively suppressed the production of nitric oxide and down-regulated inflammatory mediators confirming its anti-inflammatory effect. In conclusion, we developed a promising Nrf2 activator KDS3021 as a potential therapeutic candidate for neurodegenerative disease. We are currently testing the efficacy in animal models of Alzheimer’s and Parkinson’s disease. |
| E-mail |
217014@kist.re.kr |
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121st General Meeting of the KCS