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학술발표회초록보기

초록문의 abstract@kcsnet.or.kr

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

제112회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Hydrocarbon-Bridged α-Helix Mimetics Small Molecules

등록일
2013년 9월 5일 16시 53분 27초
접수번호
1446
발표코드
MEDI.P-961 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 16일 (수요일) 16:00~19:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
이우설, 임현석*
포항공과대학교 화학과, Korea
The α-helix-mediated protein-protein interactions (PPIs) are considered one of the most important focus in chemical biology and medicinal chemistry. Because many cellular events occur via protein-protein interaction (PPI) where protein secondary structure, such as α-helix or β-turn, plays an important role as a recognition motif. Previously, we constructed a one-bead-one-compound (OBOC) combinatorial library of triazind-piperazine-triazine-based α-helix mimetics and found a hit compound showing low micromolar affinity to MCL-1. In this research, we modified the structure of the hit compound by macrocyclization with a series of different length of linkers (C8 - C12) to reduce rotational movement of α-helix scaffold. As the result of in vitro binding assay using fluorescence polarization (FP) method, one of those macrocyclic compounds showed higher binding affinity to MCL-1 than the original hit compound. In summary, macrocyclization of the α-helix mimetics in the view of structure-activity relationship study (SARS) might be able to give structural rigidity and enhance the inhibition for PPIs.

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