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학술발표회초록보기

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  • 09월 06일 15시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제112회 대한화학회 학술발표회, 총회 및 기기전시회 안내 A novel small molecule inducer of cellular antioxidant response

등록일
2013년 9월 23일 15시 50분 58초
접수번호
1471
발표코드
BIO.O-4 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
금 12시 : 00분
발표형식
구두발표
발표분야
생명화학 - New Frontiers in Chemical Biology
저자 및
공동저자
허우영
한국과학기술연구원(KIST) 화학 키노믹스 연구센터, Korea
Eukaryotic cells counteract oxidative and other environmental stress through the activation of Nrf2, the transcription factor that controls the expression of a host of protective enzymes by binding to the antioxidant response element (ARE). The electrophilic molecules that are able to activate Nrf2 and its downstream target genes have demonstrated therapeutic potential in carcinogen-induced tumor models. Using a high-throughput cellular screen, we discovered a class of ARE activator, which we named AI-1, that activates Nrf2 by covalently modifying Keap1, the negative regulator of Nrf2. Biochemical studies indicated that modification of Cys151 of Keap1 by AI-1 disrupted the ability of Keap1 to serve as an adaptor for Cul3-Keap1 ubiquitin ligase complex, thereby causing stabilization and transcriptional activation of Nrf2. AI-1 and its biotinylated derivative are useful pharmacological probes for investigating the molecular details of the cellular antioxidant response

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