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

제112회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Design, Synthesis, and Biological Evaluation of Phenyl-Piperazine-Triazine-Based α-Helix Mimetics [우수포스터상],[RSC 포스터상]

등록일
2013년 9월 5일 16시 54분 04초
접수번호
1448
발표코드
MEDI.P-962 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 16일 (수요일) 16:00~19:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
문희조, 이우설, 임현석*
포항공과대학교 화학과, Korea
α?Helices, which account for 30% of protein secondary structure, are involved in many protein-protein interactions (PPIs) as recognition motifs. It is, therefore, of great interest to target α-helix-mediated-PPIs by developing small molecule α-helical mimetics as a modulator of such interactions. Current α-helix mimetic small molecules have several important drawbacks such as poor water solubility and synthetic difficulty. Here we describe the design and efficient solid-phase-synthesis of phenyl-piperazine-triazine scaffold as a novel class of α-helix mimetic small molecules. Our library compounds had higher synthetic accessibility, and showed improved water solubility. Additionally, the subsequent screening of a focused library molecules identified a potent inhibitor of Mcl-1/BH3 and Bcl-XL/BH3 interaction, demonstrating their ability to act as inhibitors of α-helix-mediated PPIs. Consequently, our scaffold, along with simple synthetic route, will provide an excellent source of PPI modulators.

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