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학술발표회초록보기

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  • 02월 28일 19시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제111회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Covalent approaches to targeting cancer

등록일
2013년 3월 18일 17시 53분 08초
접수번호
1501
발표코드
KCS-6 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 14시 : 30분
발표형식
심포지엄
발표분야
[KCS-ACR joint Symposium] International Frontier Scientists Symposium on "Impact of Chemistry on Biology" hosted by KAST and co-organized by KCS & ACR
저자 및
공동저자
Heather E. Beck, Bernadette V. Marquez1, Tololupe Aweda1, Claude Meares
Chemistry Department, University of California, Davis, California USA, United States
1Mallinckrodt Institute of Radiology, Washington University, St. Louis, Missouri USA, United States
※ 국외소속으로 등록된 저자의 승인여부는 최소 3일이내 발표자 email로 알려드립니다.
승인 4건

Vascular endothelial growth factor (VEGF) is a small, dimeric protein important for angiogenesis, the formation of new blood vessels. The elegant phage-display studies of Fairbrother and co-workers led to peptide ligands that blocked the receptor binding of VEGF, but with approximately micromolar dissociation constants, which are much weaker than the nano- to picomolar dissociation constants of acceptable drugs. While not a widely used design concept, a ligand that binds irreversibly to its target has several potential advantages over such weakly binding reversible ligands. For reversible binding, the concentration of free ligand must be larger than the dissociation constant in order for the target to be >50% occupied; for a covalent ligand, under ideal conditions the target could be titrated with equimolar ligand. Once tagged, the target is permanently inactivated, an outcome qualitatively different from reversible binding. To create a site on a weakly binding peptide ligand that would carry a covalent labeling reagent, we replaced a residue that does not change the peptide’s affinity for VEGF, but is located within reach of a lysine side chain on the protein. We will describe the interaction of reactively tagged peptides with VEGF, including recent studies in vivo in animal models, with particular focus on a nitroaryl fluoride reagent (see figure).

Fig.1. Marquez et al., Reactive peptide for inhibiting VEGF. Bioconjugate Chem., 2012, 23 (5), pp 1080?1089


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