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학술발표회초록보기

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  • 09월 12일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제110회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Design, synthesis and biological evaluation of novel and potent protease-activated receptor 2(PAR) antagonists for treating arthritis

등록일
2012년 8월 30일 15시 59분 21초
접수번호
1404
발표코드
MEDI.P-1197 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 17일 (수요일) 16:00~19:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
차지현, 고훈영, 조남철1, 배애님2
인하대학교 화학과, Korea
1연세대학교 생명공학과, Korea
2한국과학기술연구원 생체과학연구본부, Korea
Protease-activated receptor 2 (PAR2) is the second number of a novel family of seven-transmembrane G-protein-coupled receptors, PARs. They are mainly expressed in platelets, but also on endothelial cells, myocytes and neurons. Activation of PAR2 is initiated through a proteolytic cleavage of serine proteases such as trypsin or b-tryptase from mast cells, exposing a tethered ligand domain which binds and activates the cleaved receptor. This receptor regulates various physiological functions including vasoregulation, arteriolar dilation, degranulation of mast cells and cell growth to inflammation. Initial observations of PAR2 knock-down mice indicated that the receptors may be useful therapeutic agents for the treatment of human diseases such as arthritis. Therefore, PAR-2 is targeted to develop as inflammatory joint disease drug. A novel series of 64 quinazoline and 2 pyrimidine derivatives were designed and synthesized as PAR2 antagonist. The synthesized 6-methoxy-quinazoline compounds showed reasonable inflammatory inhibition activity against various inflammatory cell lines. The detailed design, synthesis and biological evaluation of PAR2 antagonists as inflammatory joint disease drugs will be presented.

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