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학술발표회초록보기

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  • 03월 02일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제109회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Chemical Probes inspired by cellular co-factors

등록일
2012년 3월 8일 14시 46분 43초
접수번호
1583
발표코드
ORGN1-3 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 10시 : 00분
발표형식
심포지엄
발표분야
유기화학 - KCS-RSC joint symposium- Chemical Biology
저자 및
공동저자
James Dowden
School of Chemistry, University of Nottingham, United States

Cellular co-factors provide a convenient, but challenging entry point for the design of small molecules that modulate the activity of novel biological targets. For example, we are currently focussed on developing modulators of protein arginine methyltransferases (PRMTs) since they may have a defining role in epigenetic regulation of cell status. This talk will outline our development of potential PRMT inhibitors designed to occupy binding sites for the co-factor AdoMet and the arginine protein substrate, some of which were found to discriminate between two PRMT enzyme family members, PRMT1 and CARM1. [Fig.] That the molecule above inhibits PRMT1 but not CARM1 may be explained by a key difference in respective amino acids at the binding site, specifically an electrostatic interaction with Glu47 (PRMT1, salmon), but not Asn162 (CARM1, green). Docking and overlay reveals the inhibitor occupying both co-factor site and substrate channels (blue mesh) close to these divergent amino acids


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